NOVEL COMPOUND HAVING ANTICANCER ACTIVITY, AND METHOD FOR PRODUCING SAME

Abstract

The present invention pertains to a novel compound having anticancer activity, and a method for producing same, and more specifically, to a novel compound that exhibits excellent anticancer activity by inhibiting the expression of AIMP2-DX2, and a method for producing same. The compound represented by chemical formula 1 according to the present invention is highly effective in inhibiting the expression of AIMP2-DX2, and thus can be very advantageously used for the development of agents for treating various diseases, in particular cancer, caused by AIMP2-DX2.

Claims

1. A compound of formula 1 or a pharmaceutically acceptable salt thereof: ##STR00782## wherein, R1 is hydrogen; C1˜C5 straight or branched alkyl substituted or unsubstituted with one or more substituents selected from the group consisting of hydroxy, substituted or unsubstituted phenyl, mercapto, and C1˜C5 alkylthio; Indolylmethyl unsubstituted or substituted with one or more substituents selected from the group consisting of C1˜C5 alkyl, hydroxy, hydroxycarbonyl and formyl; C1˜C5 carboxymethyl; C7˜C10 hydroxyphenylalkyl; substituted or unsubstituted C3˜C8 cycloalkyl; substituted or unsubstituted C1˜C5 aminoalkyl; ##STR00783## ##STR00784## ##STR00785## ##STR00786## R2 is hydrogen; benzenesulfonyl unsubstituted or substituted with one or more substituents selected from the group consisting of C1˜C5 straight or branched alkyl, nitro group, amine group, halo, —CF.sub.3, C1˜C5 alkylcarbonylamino, —COOH, C1˜C5 alkoxy, phenyl, —OCH.sub.2Ph, hydroxy, —COOCH.sub.2Ph, C1˜C5 alkyloxycarbonyl, —CONHCH.sub.3 and nitrile; naphthalenesulfonyl; benzylsulfonyl; benzoyl unsubstituted or substituted with one or more substituents selected from the group consisting of C1˜C5 straight or branched alkyl and C1˜C5 straight or branched alkylamine groups; thiophenesulfonyl; ##STR00787## C1˜C5 alkyloxycarbonyl; or phenylaminocarbonyl, R3 is ##STR00788## ##STR00789## ##STR00790## ##STR00791## ##STR00792## ##STR00793## ##STR00794##

2. The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein R1 is indolylmethyl unsubstituted or substituted with one or more substituents selected from the group consisting of hydroxy, substituted or unsubstituted phenyl, mercapto and C1˜C5 straight or branched alkyl substituted or unsubstituted with one or more substituents selected from the group consisting of C1˜C5 alkylthio; or C1˜C5 alkyl, hydroxy, hydroxycarbonyl and formyl, wherein R2 is benzenesulfonyl unsubstituted or substituted with one or more substituents selected from the group consisting of C1˜C5 straight or branched alkyl, nitro group, amine group, halo, —CF.sub.3, C1˜C5 alkylcarbonylamino, —COOH, C1˜C5 alkoxy, phenyl, —OCH.sub.2Ph, hydroxy, —COOCH.sub.2Ph, C1˜C5 alkyloxycarbonyl, —CONHCH.sub.3 and nitrile, Wherein R3 is ##STR00795##

3. The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein R1 is hydrogen, cyclohexane, ##STR00796## ##STR00797## ##STR00798## ##STR00799##

4. The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein R2 is hydrogen, ##STR00800## ##STR00801## ##STR00802##

5. The compound according to claim 1 or a pharmaceutically acceptable salt thereof, wherein the compound of Formula 1 is (S)-4-methyl-N-(4-methyl-1-morpholino-1-oxopentan-2-yl)benzenesulfonamide, (R)-4-methyl-N-(4-methyl-1-morpholino-1-oxopentan-2-yl)benzenesulfonamide, (S)-4-methyl-N-(4-methyl-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)pentan-2-yl)benzenesulfonamide, (R)-4-methyl-N-(4-methyl-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)-Pentan-2-yl)benzenesulfonamide, (S)—N-(1-(1,1-dioxidothiomorpholino)-4-methyl-1-oxopentan-2-yl)-4-methylbenzenesulfonamide, (N—((S)-1-((R)-2-(hydroxymethyl)pyrrolidin-1-yl)-4-methyl-1-oxopentan-2-yl)-4-methylbenzenesulfonamide, (S)-4-methyl-2-(4-methylphenylsulfonamido)-N-(4-(piperidin-1-yl)phenyl)pentanamide, (S)-4-methyl-2-(4-methylphenylsulfonamido)-N-(4-(4-methylpiperidin-1-yl)phenyl) pentanamide, (S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(6-(4-methylpiperidin-1-yl)pyridin-3-yl)pentanamide, (S)-4-methyl-2-(4-methylphenylsulfonamido)-N-(6-(4-methylpiperidin-1-yl)pyrimidin-4-yl)pentanamide, (S)-4-methyl-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)pentanamide, (S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(6-morpholinopyridin-3-yl)pentanamide, (S)—N-(6-((2S,6R)-2,6-dimethylmorpholino)pyridin-3-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide, (S)—N-(3-fluoro-4-morpholinophenyl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide, (S)—N-(4-(1,1-dioxidothiomorpholino)phenyl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide, (S)-tert-butyl 4-(5-(4-methyl-2-(4-methylphenylsulfonamido)pentanamido) pyridin-2-yl)piperazine-1-carboxylate, (S)-4-methyl-2-(4-methylphenylsulfonamido)-N-(4-(pyrrolidin-1-yl)phenyl)pentanamide, (S)-4-methyl-2-(4-methylphenylsulfonamido)-N-(2-morpholinoethyl)pentanamide, (S)—N-(4-methyl-1-morpholino-1-oxopentan-2-yl)-3-nitrobenzenesulfonamide, (S)-3-amino-N-(4-methyl-1-morpholino-1-oxopentan-2-yl)benzenesulfonamide, (S)-2-(4-fluorophenylsulfonamido)-4-methyl-N-(4-morpholinophenyl)pentanamide, (S)-2-(4-bromophenylsulfonamido)-4-methyl-N-(4-morpholinophenyl)pentanamide, (S)-4-methyl-N-(4-morpholinophenyl)-2-(4-(trifluoromethyl)phenylsulfonamido)pentanamide, (S)-4-methyl-N-(4-morpholinophenyl)-2-(3-nitrophenylsulfonamido)pentanamide, (S)-4-methyl-N-(4-morpholinophenyl)-2-(naphthalene-1-sulfonamido)pentanamide, (S)-4-methyl-N-(4-morpholinophenyl)-2-(naphthalene-2-sulfonamido)pentanamide, (S)-4-methyl-N-(4-morpholinophenyl)-2-(phenylsulfonamido)pentanamide, (S)-Benzyl 4-methyl-2-(3-(phenylsulfonyl)propanamido)pentanoate, (S)-2-(4-methoxyphenylsulfonamido)-4-methyl-N-(4-morpholinophenyl)pentanamide, (S)-4-methyl-N-(4-morpholinophenyl)-2-(thiophene-2-sulfonamido)pentanamide, (S)-4-methyl-N-(4-morpholinophenyl)-2-(4-nitrophenylsulfonamido)pentanamide, (S)-2-(4-isopropylphenylsulfonamido)-4-methyl-N-(4-morpholinophenyl)pentanamide, (S)-2-(biphenyl-4-ylsulfonamido)-4-methyl-N-(4-morpholinophenyl)pentanamide, (S)-4-(benzyloxy)-N-(4-methyl-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)pentan-2-yl)benzenesulfonamide, (S)-4-hydroxy-N-(4-methyl-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)pentan-2-yl)benzenesulfonamide, (S)-benzyl 4-(N-(4-methyl-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)pentan-2-yl)sulfamoyl)benzoate, (S)-tert-butyl 3-(4-methylphenylsulfonamido)-4-morpholino-4-oxobutanoate, (S)-4-methyl-N-(1-morpholino-1-oxo-3-phenylpropan-2-yl)benzenesulfonamide, (S)—N-(3-hydroxy-1-morpholino-1-oxopropan-2-yl)-4-methylbenzenesulfonamide, (S)-4-methyl-N-(3-methyl-1-morpholino-1-oxobutan-2-yl)benzenesulfonamide, (R)—N-(3-mercapto-1-morpholino-1-oxopropan-2-yl)-4-methylbenzenesulfonamide, (2S,3S)-3-hydroxy-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)butanamide, (2S,3S)-3-methyl-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)pentanamide, (S)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (S)-2-(4-methylphenylsulfonamido)-4-(methylthio)-N-(4-morpholinophenyl)butanamide, (S)-3-(1H-indol-2-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl) propanamide, (S)-3-(1-methyl-1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl) propanamide, (S)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)-3-phenylpropanamide, (S)-benzyl 4-methyl-2-(4-methylphenylsulfonamido)pentanoate, (S)-benzyl 4-methyl-2-(4-methylbenzamido)pentanoate, (S)-benzyl 2-(4-tert-butylbenzamido)-4-methylpentanoate, (S)-benzyl 2-(benzo[d][1,3]dioxole-5-carboxamido)-4-methylpentanoate, (S)-benzyl 2-(4-(tert-butoxycarbonylamino)benzamido)-4-methylpentanoate, (S)-benzyl 4-methyl-2-(3-(phenylsulfonyl)propanamido)pentanoate, (S)—N-(4-(4-methoxyphenyl)thiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide, (S)-1-(4-methyl-1-morpholino-1-oxopentan-2-yl)-3-phenylurea, (S)-4-tert-butyl-N-(4-methyl-1-morpholino-1-oxopentan-2-yl)benzamide, (S)—N-(4-methyl-1-morpholino-1-oxopentan-2-yl)-3-(phenylsulfonyl)propanamide, (S)-4-tert-butyl-N-(4-methyl-1-(4-morpholinophenylamino)-1-oxopentan-2-yl)benzamide, (S)—N-(4-methyl-1-(4-morpholinophenylamino)-1-oxopentan-2-yl)benzo[d][1,3]dioxole-5-carboxamide, (S)-4-methyl-N-(4-morpholinophenyl)-2-(3-(phenylsulfonyl)propanamido)pentanamide, (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide, (S)-3-(1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-2-(4-methylphenylsulfonamido)propanamide, (S)-3-(1H-indol-3-yl)-2-(2-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (S)-3-(1H-indol-3-yl)-2-(3-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (S)-2-(3,5-dimethylphenylsulfonamido)-3-(1H-indol-3-yl)-N-(4 morpholinophenyl)propanamide, (S)-2-(4-Fluorophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propanamide, (S)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)-2-(4-(trifluoromethyl)phenylsulfon-amido)propanamide, (S)-3-(5-Hydroxy-1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (S)—N-(3-(1H-indol-3-yl)-1-morpholino-1-oxopropan-2-yl)-4-methylbenzenesulfonamide, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(5-morpholinothiazol-2-yl)propan amide, (S)-2-(2,4-dimethylphenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propanamide, 3-(3-ethoxy-2-(4-methylphenylsulfonamido)-3-oxopropyl)-1H-indole-5-carboxylic acid, (S)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)-3-(1-tosyl-1H-imidazol-4-yl)propanamide, (S)—N-(6-((2S,6R)-2,6-dimethylmorpholino)pyridin-3-yl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propenamide, (R)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (S)—N-(3-fluoro-4-morpholinophenyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide, (S)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)-2-(4-nitrophenylsulfonamido)propanamide, (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propanamide, (S)-3-(1H-indol-3-yl)-2-(4-methoxyphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (S)-3-(1H-indol-3-yl)-2-(4-isopropylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (S)-3-(1H-indol-3-yl)-2-(4-isopropylphenylsulfonamido)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propenamide, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-methylthiazol-2-yl)propanamide, (S)—N-(benzo[d]thiazol-2-yl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide, (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)propanoic acid, (S)-4-methyl-2-(4-methylphenylsulfonamido)-N-(5-morpholinothiazol-2-yl)pentanamide, (S)—N-(5-(4-methoxyphenyl)-1,3,4-thiadiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide, (S)—N-(5-(4-methoxyphenyl)isoxazol-3-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide, (S)—N-(3-(4-methoxyphenyl)isoxazol-5-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide, (S)-4-methyl-2-(4-methylphenylsulfonamido)-N-(4-(4-(trifluoromethyl)phenyl)thiazol-2-yl)pentanamide, (S)—N-(4-(3,4-dimethoxyphenyl)thiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide, (S)—N-(4-(2-bromo-4-fluorophenyl)thiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide, (S)-4-(2-aminothiazol-4-yl)phenyl-4-methyl-2-(4-methylphenylsulfonamido)pentanoate, (S)—N-(4-(4-fluorophenyl)thiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide, (S)-4-methyl-2-(4-methylphenylsulfonamido)-N-(4-(4-(trifluoromethoxy)phenyl)thiazol-2-yl)pentanamide, (S)—N-(4-(4-hydroxyphenyl)thiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide (S)-4-methyl-2-(4-methylphenylsulfonamido)-N-(4-p-tolylthiazol-2-yl)pentanamide, (S)—N-(4-(4-((S)-1-methoxypropan-2-yloxy)phenyl)thiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide, (S)-4-methyl-2-(4-methylphenylsulfonamido)-N-(4-(4-morpholinophenyl)thiazol-2-yl)pentanamide, (S)-methyl-4-(2-(4-methyl-2-(4-methylphenylsulfonamido)pentanamido)thiazol-4-yl)benzoate, (S)-4-(2-(4-methylphenylsulfonamido)-3-(4-morpholinophenylamino)-3-oxopropyl)phenyl 4-methylbenzenesulfonate, (S)-2-(4-bromophenylsulfonamido)-3-(1H-imidazol-4-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide, (S)—N-methoxy-N,4-dimethyl-2-(4-methylphenylsulfonamido)pentanamide, (S)-3-(1H-indol-3-yl)-N-methoxy-N-methyl-2-(4-methylphenylsulfonamido)propanamide, (S)—N-(3-(1H-indol-3-yl)-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)propan-2-yl)-4-methylbenzenesulfonamide, (S)-2-(4-tert-butylphenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propan amide, (S)-2-(4-bromophenylsulfonamido)-N-(4-(2-chlorophenyl)thiazol-2-yl)-3-(1H-indol-3-yl)propanamide, (S)-2-(4-bromophenylsulfonamido)-N-(4-(2,4-dimethoxyphenyl)thiazol-2-yl)-3-(1H-indol-3-yl)propanamide, (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(thiazol-2-yl)propanamide, (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(5-methylthiazol-2-yl)propanamide, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-methylthiazol-2-yl)propanamide, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(5-methylthiazol-2-yl)propanamide, (S)-methyl 4-(N-(3-(1H-indol-3-yl)-1-(4-morpholinophenylamino)-1-oxopropan-2-yl)sulfamoyl)benzoate, (S)-ethyl 4-(N-(3-(1H-indol-3-yl)-1-(4-morpholinophenylamino)-1-oxopropan-2-yl)sulfamoyl)benzoate, (S)-3-(4-benzoylphenyl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (S)-4-(N-(3-(1H-indol-3-yl)-1-(4-morpholinophenylamino)-1-oxopropan-2-yl)sulfamoyl)-N-methylbenzamide, (S)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)-3-(naphthalen-2-yl)propanamide, (S)-tert-butyl 3-(1H-indol-3-yl)-1-(4-morpholinophenylamino)-1-oxopropan-2-ylcarbamate, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanoic acid, (S)-tert-butyl-4-(4-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)-3-methoxyphenyl)piperazine-1-carboxylate, (S)-3-(1H-indol-3-yl)-N-(2-methoxy-4-(piperazin-1-yl)phenyl)-2-(4-methylphenylsulfonamido)propanamide, (S)-tert-butyl-4-(4-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)phenyl)piperazine-1-carboxylate, (S)-3-(1H-indol-3-yl)-N-(2-methoxy-4-morpholinophenyl)-2-(4-methylphenylsulfonamido)propanamide, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-(piperazin-1-yl)phenyl)propanamide, (S)-3-(1-formyl-1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (S)-3-(1H-indol-3-yl)-N-(3-(4-methoxyphenyl)isoxazol-5-yl)-2-(4-methylphenylsulfonamido)propanamide, (S)-benzyl 3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanoate, (S)-benzyl 3-(1H-indol-3-yl)-2-(4-methylbenzamido)propanoate, (S)—N-(3-(1H-indol-3-yl)-1-(4-morpholinophenylamino)-1-oxopropan-2-yl)-4-methylbenzamide, (S)-3-hydroxy-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (S)-3-methyl-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)butanamide, (S)-1-(3-(1H-indol-3-yl)-1-morpholino-1-oxopropan-2-yl)-3-phenylurea, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(6-morpholinopyridin-3-yl)propanamide, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(2-morpholinopyrimidin-5-yl)propanamide, (S)-2-(4-cyanophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propanamide, (S)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)-2-(6-(trifluoromethyl)pyridine-3-sulfonamido)propanamide, (S)-methyl 4-(4-methylphenylsulfonamido)-5-(4-morpholinophenylamino)-5-oxopentanoate, (S)-3-(1H-benzo[d]imidazol-1-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (R)-3-(2,3-dioxo-3,4-dihydroquinoxalin-1(2H)-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide, (S)—N-(5-(4-methylphenylsulfonamido)-6-(4-morpholinophenylamino)-6-oxohexyl)-5-(trifluoromethyl)picolinamide, (S)-benzyl 4-(4-methylphenylsulfonamido)-5-(4-morpholinophenylamino)-5-oxopentanoate, (S)-benzyl 3-(4-methylphenylsulfonamido)-4-(4-morpholinophenylamino)-4-oxobutanoate, (S)-4-methyl-N-(4-methyl-1-(4-morpholinophenylamino)-1-oxopentan-2-yl)benzamide, 2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)acetamide, (S)-3-(4-methylphenylsulfonamido)-4-(4-morpholinophenylamino)-4-oxobutanoic acid, (S)-4-(4-methylphenylsulfonamido)-5-(4-morpholinophenylamino)-5-oxopentanoic acid, (S)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)-3-phenylpropanamide, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-phenylpropanamide, (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-phenylpropanamide, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(thiophen-2-ylmethyl)propanamide, (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(thiophen-2-ylmethyl)propanamide, (S)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(2-methoxyphenyl)thiazol-2-yl)propanamide, (S)—N-(3-(N-(4-methyl-1-morpholino-1-oxopentan-2-yl)sulfamoyl)phenyl)acetamide, (S)-Benzyl 4-methyl-2-(3-phenylureido)pentanoate, 4-Methyl-N-(2-morpholino-2-oxoethyl)benzenesulfonamide, 4-Methyl-N-(1-(morpholine-4-carbonyl)cyclohexyl)benzenesulfonamide, (S)-4-(N-(4-methyl-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)pentan-2-yl)sulfamoyl)benzoic acid, (S)-2-(4-Hydroxyphenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propenamide, (S)-4-(N-(3-(1H-indol-3-yl)-1-(4-morpholinophenylamino)-1-oxopropan-2-yl)sulfamoyl)benzoic acid, (S)-2-Amino-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propenamide, (S)—N-(4-(4-Acetylpiperazin-1-yl)-2-methoxyphenyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propenamide, (S)—N-(4-(4-Acetylpiperazin-1-yl)phenyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propenamide, (S)—N-(3-(1H-indol-3-yl)-1-(2-(4-morpholinobenzoyl)hydrazinyl)-1-oxopropan-2-yl)-4-methylbenzenesulfonamide, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-(4-morpholinophenyl)thiazol-2-yl)propanamide, (S)-Methyl-4-(2-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)thiazol-4-yl)benzoate, (S)-Benzyl-3-(1H-indol-3-yl)-2-(6-(trifluoromethyl)pyridine-3-sulfonamido)propanoate, (S)-2-(4-Methylphenylsulfonamido)-N.sup.1-(4-morpholinophenyl)-N.sup.5-(4-nitrophenyl)pentanediamide, (S)-Benzyl-5-(4-methylphenylsulfonamido)-6-(4-morpholinophenylamino)-6-oxohexylcarbamate, (S)-6-Amino-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)hexanamide, (S)-3,5-Dimethoxy-N-(5-(4-methylphenylsulfonamido)-6-(4-morpholinophenylamino)-6-oxohexyl)benzamide, (S)—N.sup.5-(4-Methoxybenzyl)-2-(4-methylphenylsulfonamido)-N.sup.1-(4-morpholinophenyl)pentanediamide, (S)-2-(4-Methylphenylsulfonamido)-N.sup.1-(4-morpholinophenyl)-N.sup.5-phenylpentanediamide, (S)-2-(4-Methylphenylsulfonamido)-5-morpholino-N-(4-morpholinophenyl)-5-oxopentanamide, S)—N.sup.5-(4-fluorophenyl)-2-(4-methylphenylsulfonamido)-N.sup.1-(4-morpholinophenyl)pentanediamide, (S)—N-(4-tert-butylphenyl)-2-(4-methylphenylsulfonamido)-N.sup.1-(4-morpholinophenyl)pentanediamide, (S)-2-(4-Methylphenylsulfonamido)-N.sup.1-(4-morpholinophenyl)-N.sup.5-(4-(trifluoromethyl)phenyl)pentanediamide, (S)-2-(4-Methylphenylsulfonamido)-N.sup.1-(4-morpholinophenyl)-N.sup.4-(4-nitrophenyl)succinamide, (S)—N-(furan-2-ylmethyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide, (S)-2-(4-Bromophenylsulfonamido)-N-(furan-2-ylmethyl)-3-(1H-indol-3-yl)propanamide, (S)-3-(1H-indol-3-yl)-N-isopropyl-2-(4-methylphenylsulfonamido)propanamide, (S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-isopropylpropanamide, (S)—N-(3-(1H-indol-3-yl)-1-(2-(4-methoxybenzoyl)hydrazinyl)-1-oxopropan-2-yl)-4-methylbenzenesulfonamide, (S)-2-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanoyl)-N-(4-methoxyphenyl)hydrazinecarboxamide, (S)-4-Bromo-N-(1-(3,5-dimethyl-1H-pyrazol-1-yl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)benzenesulfonamide, (S)—N-(3-(1H-indol-3-yl)-1-oxo-1-(3-phenyl-1H-pyrazol-1-yl)propan-2-yl)-4-bromobenzenesulfonamide, N—((S)-1-(2-((3S,5S,7S)-adamantane-1-carbonyl)hydrazinyl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-4-methylbenzenesulfonamide, (S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(p-tolyl)thiazol-2-yl)propanamide, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-phenethylpropanamide, (S)-2-(4-Bromophenylsulfonamido)-N-(4-(4-fluorophenyl)thiazol-2-yl)-3-(1H-indol-3-yl)propanamide, (S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(4-nitrophenyl)thiazol-2-yl)propanamide, (S)—N-(3-(1H-indol-3-yl)-1-(2-(4-methoxybenzoyl)hydrazinyl)-1-oxopropan-2-yl)-4-methylbenzenesulfonamide, (S)-2-(4-Bromophenylsulfonamido)-N-(4-(4-cyanophenyl)thiazol-2-yl)-3-(1H-indol-3-yl)propanamide, (S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(4-(trifluoromethyl)phenyl)thiazol-2-yl)propanamide, (S)-4-Bromo-N-(1-(2-dodecanoylhydrazinyl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)benzenesulfonamide, (S)-4-Bromo-N-(1-(2-decanoylhydrazinyl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)benzenesulfonamide, (S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-phenethylpropanamide, N—((S)-1-(2-((3S,5S,7S)-adamantane-1-carbonyl)hydrazinyl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-4-bromobenzenesulfonamide, (S)-2-(4-Bromophenylsulfonamido)-N-(4-fluorophenethyl)-3-(1H-indol-3-yl)propanamide, (S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-methoxyphenethyl)propanamide, (S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(3-phenylpropyl)propanamide, (S)—N-((3R,5R,7R)-adamantan-1-yl)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)propanamide, (S)—N-(3-(1H-indol-3-yl)-1-(4-(4-methoxyphenyl)piperazin-1-yl)-1-oxopropan-2-yl)-4-bromobenzenesulfonamide, (S)—N-(3-(1H-indol-3-yl)-1-(4-(4-methoxyphenyl)piperazin-1-yl)-1-oxopropan-2-yl)-4-methylbenzenesulfonamide, (S)—N-((3R,5R,7R)-adamantan-1-yl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide, (S)-3-(1H-indol-3-yl)-N-(4-methoxyphenethyl)-2-(4-methylphenylsulfonamido)propanamide, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(3-phenylpropyl)propanamide, (S)—N-(4-fluorophenethyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide, (S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-(4-(trifluoromethyl)phenyl)thiazol-2-yl)propanamide, (S)—N-(2-(1H-indol-3-yl)ethyl)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)propanamide, (S)—N-(3-(1H-indol-3-yl)-1-((4-(4-methoxyphenyl)thiazol-2-yl)amino)-1-oxopropan-2-yl)-4-methylbenzamide, (S)-2-(4-Chlorophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide, (S)-3-(1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-2-(4-(trifluoromethyl)phenylsulfonamido)propanamide, (S)-2-(4-Fluorophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide, (S)-2-(4-Bromophenylsulfonamido)-N-((1r,3R,5S,7S)-3,5-dimethyladamantan-1-yl)-3-(1H-indol-3-yl)propanamide, (S)-2-(4-Cyanophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide, (S)-Benzyl 3-(1H-indol-3-yl)-2-(4-methylbenzamido)propanoate, (S)-2-(4-Bromophenylsulfonamido)-3-(5-hydroxy-1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide, (S)-2-(4-Bromophenylsulfonamido)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-3-(5-methyl-1H-indol-3-yl)propenamide, (S)-2-(4-Bromophenylsulfonamido)-3-(5-fluoro-1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide, (S)-4-(2-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)ethyl)benzoic acid, (S)—N-(4-bromophenethyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide, (S)—N-(2-(1H-indol-3-yl)ethyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propenamide, (S)-3-(1H-indol-3-yl)-N-(4-methylphenethyl)-2-(4-methylphenylsulfonamido)propanamide, Ethyl 2-((S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)-3-(1H-indol-3-yl)propanoate, (S)—N-(4-chlorophenethyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide, 2-((S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)-3-(1H-indol-3-yl)propanoic acid, (S)-Methyl-4-(2-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)thiazol-4-yl)benzoate, (S)-4-(2-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)thiazol-4-yl)benzoic acid, (S)-3-(Benzo[d]oxazol-2-ylamino)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-2-(4-methylphenylsulfonamido)propanamide, (S)—N-(3-((4-(4-methoxyphenyl)thiazol-2-yl)amino)-2-(4-methylphenylsulfonamido)-3-oxopropyl)benzamide, (S)—N-(3-((4-(4-methoxyphenyl)thiazol-2-yl)amino)-2-(4-methylphenylsulfonamido)-3-oxopropyl)nicotinamide or (S)—N-(3-((4-(4-methoxyphenyl)thiazol-2-yl)amino)-2-(4-methylphenylsulfonamido)-3-oxopropyl)pyrimidine-5-carboxamide.

6. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein the compound inhibits the expression of AIMP2-DX2.

7. A method for preparing the compound of claim 1 or a pharmaceutically acceptable salt thereof prepared by the following Reaction Formula: <Reaction Formula 1> ##STR00803## wherein R1, R2 and R3 are as defined in claim 1.

8. A pharmaceutical composition comprising a compound of claim 1 or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable carriers, excipients, or diluents.

9-12. (canceled)

13. A method for treating cancer comprising administering to a subject in need thereof an effective amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof.

14. (canceled)

15. A method for treating an inflammatory disease comprising administering to a subject in need thereof an effective amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof.

16. The method of claim 13, wherein the cancer is selected from the group consisting of leukemia, brain tumor, kidney cancer, stomach cancer, skin cancer, bladder cancer, breast cancer, uterine cancer, melanoma, thyroid cancer, head and neck cancer, lymphoma, gallbladder cancer, esophageal cancer, lung cancer, colon cancer, prostate cancer, ovarian cancer, liver cancer, colorectal cancer, peritoneal cancer, peritoneal metastatic cancer and pancreatic cancer.

17. The method of claim 15, wherein the inflammatory disease is selected from the group consisting of inflammatory skin diseases, crohn's disease, ulcerative colitis, peritonitis, osteomyelitis, cellulitis, meningitis, encephalitis, pancreatitis, trauma-induced shock, bronchial asthma, allergic rhinitis, cystic fibrosis, stroke, acute bronchitis, chronic bronchitis, acute bronchiolitis, chronic bronchiolitis, osteoarthritis, gout, spondyloarthropathy, ankylosing spondylitis, Reiter's syndrome, psoriatic arthropathy, enteric spondylitis, juvenile arthropathy, juvenile ankylosing spondylitis, reactive arthropathy, infectious arthritis, post-infectious arthritis, gonococcal arthritis, tuberculous arthritis, viral arthritis, fungal arthritis, syphilitic arthritis, Lyme disease, arthritis associated with ‘vasculitis syndrome’, polyarteritis nodosa, hypersensitivity vasculitis, Lou Gehrig's granulomatosis, polymyalgia rheumatica, articular cell arteritis, calcium crystals deposited arthropathy, pseudo gout, non-articular rheumatism, bursitis, tendinitis, epicondylitis (tennis elbow), neuropathic joint disease (charco and joint), hemarthrosic, Henoch-Schonlein purpura, hypertrophic osteoarthropathy, multicentral reticulocytoma, surcoilosis, hemochromatosis, sickle cell disease and other hemoglobinopathy, hyperproteinemia, hypogammaglobulinemia, familial thalassemia, Behat's disease, systemic lupus erythematosus, relapsing fever, psoriasis, multiple sclerosis, sepsis, septic shock, multiple organ dysfunction syndrome, acute respiratory distress syndrome, chronic obstructive pulmonary disease, rheumatoid arthritis, acute lung injury and broncho-pulmonary dysplasia.

Description

BRIEF DESCRIPTION OF THE DRAWINGS

[0314] FIG. 1 is a result of calculating the IC50 for AIMP2-DX2 and AIMP2 by measuring the fluorescence after treating nanoruciferase-DX2 or -AIMP2-expressing A549 cells with compound No. 63 of the present invention for 4 hours at each concentration.

[0315] FIG. 2 is a result confirming through an in vitro pull-down assay that compound No. 63 of the present invention inhibits the binding of AIMP2-DX2 and HPS70. After mixing the purified AIMP2-DX2-His6 and HSP70 proteins and treating compound No. 63 for 4 hours at each concentration, AIMP2-DX2 was precipitated with Ni-IDA resin, and HSP70 precipitated with AIMP2-DX2 was visualized by SDS-PAGE and Coomassie staining.

[0316] FIGS. 3a to 3d are the results of observing the tumor growth while administering compound No. 63 (50 mg/kg) once every two days intraperitoneally for a total of 15 days to a mouse transplanted with H460 cells. (FIG. 3a: macroscopic observation of each mouse and tumor after the end of administration, FIG. 3b: tumor growth curve over time, FIG. 3c: the weight of each tumor obtained at the end of administration, FIG. 3d: change in body weight of animals during administration period).

[0317] FIG. 4 is a result of testing the cancer cell growth inhibitory effect of compound No. 55 and compound No. 89 among the compounds of the Formula 1 according to the present invention and the tumor distribution of the drug in the H460 xenograft animal model. Taxol was used as a positive control.

MODE FOR CARRYING OUT INVENTION

[0318] Hereinafter, the present invention will be described in detail.

[0319] However, the following examples are only illustrative of the present invention, and the content of the present invention is not limited to the following examples.

Example 1: Preparation of Compounds

[0320] In the present invention, the compound of Formula 1 was prepared according to the following Reaction Formula 1:

[0321] [Reaction Formula 1]

##STR00781##

[0322] In the Reaction Formula, R1, R2 and R3 are as defined above.

[0323] Specifically, starting materials, acid (1) (1.0 eq.), 2M NaOH solution (1.0 eq.) were taken. The mixture was stirred at 0° C. for several minutes until a clear solution was formed. To the above solution were added sulfonyl chloride (1.05 eq.), DIPEA (1.1 eq.) and acetone. The mixture was stirred at 0° C. for 10 min and then at room temperature for 12 h. After completion of the reaction, the mixture was washed with ether to remove organic impurities. The combined organic layers were washed again with 2M NaOH. To the aqueous layer was added 2N HCl at 0° C. until the pH was 2. Then the whole aqueous mixture was extracted with ethyl acetate, water and brine. The organic solvent was dried over MgSO.sub.4 and evaporated in vacuo to obtain compound (2).

[0324] To 15 mL of DMF or DCM:THF=1:1 was added the above compound (2) (2 eq.), amine (1.1 eq.), EDCl (1.1 eq.) and HOBt (1.1 eq.). The mixture was stirred at room temperature overnight, then extracted with ethyl acetate, water and brine. The organic layer was dried over MgSO.sub.4 and evaporated in vacuo to obtain a crude product of compound (3), which was purified by column chromatography to obtain pure compound (3).

[0325] Specific examples, structures, and NMR analysis results of the compound of the Formula 1 prepared according to the above method are shown below in detail.

(S)-4-Methyl-N-(4-methyl-1-morpholino-1-oxopentan-2-yl)benzenesulfonamide

[0326] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.70 (d, J=8.40 Hz, 2H), 7.29 (d, J=8.00 Hz, 2H), 5.74 (d, J=9.60 Hz, 1H), 4.06-4.01 (m, 1H), 3.61-3.51 (m, 2H), 3.41-3.36 (m, 1H), 3.31-3.14 (m, 5H), 2.42 (s, 3H), 2.00-1.93 (m, 1H), 1.50-1.43 (m, 1H), 1.17-1.11 (m, 1H), 0.95 (d, J=6.80 Hz, 3H), 0.92 (d, J=6.80 Hz, 3H)

(R)-4-methyl-N-(4-methyl-1-morpholino-1-oxopentan-2-yl)benzenesulfonamide

[0327] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.70 (d, J=8.80 Hz, 2H), 7.29 (d, J=8.40 Hz, 2H), 5.78 (d, J=9.60 Hz, 1H), 4.08-4.02 (m, 1H), 3.59-3.42 (m, 2H), 3.41-3.32 (m, 1H), 3.31-3.15 (m, 5H), 2.41 (s, 3H), 1.99-1.92 (m, 1H), 1.50-1.42 (m, 1H), 1.19-1.12 (m, 1H), 0.95 (d, J=6.80 Hz, 3H), 0.92 (d, J=6.80 Hz, 3H)

(S)-4-Methyl-N-(4-methyl-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)pentan-2-yl)benzenesulfonamide

[0328] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.71 (d, J=8.00 Hz, 2H), 7.27 (d, J=8.00 Hz, 2H), 5.59 (d, J=10.0 Hz, 1H), 4.25-4.19 (m, 1H), 3.78-3.71 (m, 2H), 3.69-3.37 (m, 11H), 3.22-3.12 (m, 3H), 2.40 (s, 3H), 1.98-1.91 (m, 1H), 1.49-1.33 (m, 2H), 0.91 (t, J=6.00 Hz, 6H)

(R)-4-methyl-N-(4-methyl-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)-Pentan-2-yl)benzenesulfonamide

[0329] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.71 (d, J=8.00 Hz, 2H), 7.27 (d, J=8.40 Hz, 2H), 5.66 (d, J=9.60 Hz, 1H), 4.26-4.20 (m, 1H), 3.79-3.67 (m, 2H), 3.66-3.38 (m, 11H), 3.23-3.12 (m, 3H), 2.40 (s, 3H), 1.97-1.90 (m, 1H), 1.49-1.33 (m, 2H), 0.92 (d, J=4.20 Hz, 3H), 0.89 (d, J=5.60 Hz, 3H)

(S)—N-(1-(1,1-dioxidothiomorpholino)-4-methyl-1-oxopentan-2-yl)-4-methylbenzenesulfonamide

[0330] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.73 (d, J=7.60 Hz, 2H), 7.34 (d, J=7.60 Hz, 2H), 5.59 (d, J=9.60 Hz, 1H), 4.40 (d, J=14.0 Hz, 1H), 4.05-3.99 (m, 1H), 3.81 (d, J=14.8 Hz, 1H), 3.66 (t, J=12.6 Hz, 1H), 3.32 (t, J=12.2 Hz, 1H), 2.88 (t, J=11.2 Hz, 2H), 2.61-2.56 (m, 1H), 2.50-2.40 (m, 4H), 1.97-1.92 (m, 1H), 1.52-1.46 (m, 1H), 1.22-1.16 (m, 1H), 0.93 (d, J=6.40 Hz, 3H), 0.85 (d, J=6.40 Hz, 3H)

N—((S)-1-((R)-2-(hydroxymethyl)pyrrolidin-1-yl)-4-methyl-1-oxopentan-2-yl)-4-methylbenzenesulfonamide

[0331] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.70 (d, J=8.20 Hz, 2H), 7.28 (d, J=7.60 Hz, 2H), 5.60 (d, J=9.60 Hz, 1H), 4.05 (dd, J=3.00, 7.40 Hz, 1H), 3.97-3.91 (m, 1H), 4.06-4.03 (m, 1H), 3.97-3.91 (m, 1H), 3.63-3.61 (m, 1H), 3.52-3.49 (m, 1H), 3.29-3.25 (m, 2H), 2.42 (s, 3H), 1.94-1.85 (m, 2H), 1.77-1.68 (m, 2H), 1.56-1.47 (m, 2H), 1.25-1.19 (m, 1H), 0.94 (d, J=3.20 Hz, 3H), 0.93 (d, J=4.00 Hz, 3H)

(S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(4-(piperidin-1-yl)phenyl)pentanamide

[0332] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.85 (s, 1H), 7.76 (d, J=8.00 Hz, 2H), 7.22-7.12 (m, 4H), 6.82-6.78 (m, 2H), 5.48 (s, 1H), 3.84-3.82 (m, 1H), 3.07 (t, J=5.60 Hz, 4H), 2.32 (s, 3H), 1.71-1.46 (m, 8H), 0.85 (d, J=6.00 Hz, 3H), 0.72 (d, J=5.60 Hz, 3H)

(S)-Methyl-2-(4-methylphenylsulfonamido)-N-(4-(4-methylpiperidin-1-yl)phenyl) pentanamide

[0333] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.97 (s, 1H), 7.76 (d, J=8.00 Hz, 2H), 7.21-7.12 (m, 4H), 6.81-6.77 (m, 2H), 5.66 (d, J=7.60 Hz, 1H), 3.88-3.83 (m, 1H), 3.56-3.53 (m, 2H), 2.65-2.58 (m, 2H), 2.31 (s, 3H), 1.73-1.70 (m, 2H), 1.62-1.56 (m, 2H), 1.50-1.45 (m, 2H), 1.37-1.25 (m, 2H), 0.97 (d, J=6.40 Hz, 3H), 0.84 (d, J=6.00 Hz, 3H), 0.71 (d, J=5.60 Hz, 3H)

(S)-Methyl-2-(4-methylphenylsulfonamido)-N-(6-(4-methylpiperidin-1-yl)pyridin-3-yl)pentanamide

[0334] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.21 (s, 1H), 7.98 (d, J=2.80 Hz, 1H), 7.76 (d, J=8.40 Hz, 2H), 7.48 (dd, J=2.80, 8.80 Hz, 1H), 7.22 (d, J=8.00 Hz, 2H), 6.52 (d, J=8.80 Hz, 1H), 5.85 (d, J=8.00 Hz, 1H), 4.16-4.11 (m, 2H), 3.91-3.86 (m, 1H), 2.78-2.72 (m, 2H), 2.32 (s, 3H), 1.69-1.47 (m, 6H), 1.23-1.13 (m, 2H), 0.95 (d, J=6.00 Hz, 3H), 0.83 (d, J=6.40 Hz, 3H), 0.68 (d, J=6.40 Hz, 3H)

(S)-Methyl-2-(4-methylphenylsulfonamido)-N-(6-(4-methylpiperidin-1-yl)pyrimidin-4-yl)pentanamide

[0335] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.76 (s, 1H), 8.31 (s, 1H), 7.75 (d, J=8.40 Hz, 2H), 7.22 (d, J=8.40 Hz, 3H), 6.21 (s, 2H), 4.37 (s, 2H), 3.85 (s, 1H), 2.90-2.84 (m, 2H), 2.31 (s, 3H), 1.80-1.60 (m, 4H), 1.53-1.1.47 (m, 2H), 1.19-1.09 (m, 2H), 0.97 (d, J=6.80 Hz, 3H), 0.82 (d, J=6.80 Hz, 3H), 0.70 (d, J=6.40 Hz, 3H)

(S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl) pentanamide

[0336] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.95 (s, 1H), 7.76 (d, J=8.00 Hz, 2H), 7.28-7.16 (m, 4H), 6.84-6.71 (m, 2H), 5.49 (d, J=7.60 Hz, 1H), 3.84 (t, J=4.80 Hz, 4H), 3.08 (t, J=4.80 Hz, 4H), 2.33 (s, 3H), 1.60-1.58 (m, 2H), 1.50-1.46 (m, 1H), 0.84 (d, J=6.00 Hz, 3H), 0.70 (d, J=5.60 Hz, 3H)

(S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(6-morpholinopyridin-3-yl)pentanamide

[0337] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.29 (s, 1H), 8.04 (d, J=2.40 Hz, 1H), 7.77 (d, J=8.40 Hz, 2H), 7.59 (dd, J=2.80, 9.20 Hz, 1H), 7.23 (d, J=8.40 Hz, 2H), 6.52 (d, J=8.80 Hz, 1H), 5.90 (d, J=8.00 Hz, 1H), 3.92-3.86 (m, 1H), 3.80 (t, J=5.00 Hz, 4H), 3.42 (t, J=4.60 Hz, 4H), 2.34 (s, 3H), 1.60-1.48 (m, 3H), 0.83 (d, J=6.00 Hz, 3H), 0.67 (d, J=6.00 Hz, 3H)

(S)—N-(6-((2S,6R)-2,6-dimethylmorpholino)pyridin-3-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide

[0338] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.03 (d, J=2.40 Hz, 2H), 8.00 (s, 1H), 7.77 (d, J=8.40 Hz, 2H), 7.61 (dd, J=2.80, 9.20 Hz, 1H), 7.26 (d, J=8.00 Hz, 2H), 6.53 (d, J=9.20 Hz, 1H), 5.48 (d, J=7.60 Hz, 1H), 4.13 (q, J=7.20 Hz, 1H), 3.95 (dd, J=2.00, 12.8 Hz, 2H), 3.87-3.82 (m, 1H), 3.72-3.68 (m, 2H), 2.49-2.44 (m, 2H), 2.35 (s, 3H), 1.63-1.58 (m, 2H), 1.52-1.47 (m, 1H), 1.25 (d, J=8.00 Hz, 6H), 0.85 (d, J=6.00 Hz, 3H), 0.69 (d, J=6.40 Hz, 3H)

(S)—N-(3-fluoro-4-morpholinophenyl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide

[0339] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.81 (s, 1H), 7.76 (d, J=8.00 Hz, 2H), 7.29 (d, J=8.00 Hz, 2H), 7.26-7.21 (m, 1H), 6.98 (d, J=6.00 Hz, 1H), 6.85 (t, J=9.00 Hz, 1H), 4.90 (d, J=7.20 Hz, 1H), 3.86 (t, J=4.60 Hz, 4H), 3.77-3.72 (m, 1H), 3.04 (t, J=4.40 Hz, 4H), 2.38 (s, 3H), 1.67-1.43 (m, 3H), 0.86 (d, J=6.40 Hz, 3H), 0.68 (d, J=6.40 Hz, 3H)

(S)—N-(4-(1,1-dioxidothiomorpholino)phenyl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide

[0340] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.07 (s, 1H), 7.78 (d, J=8.40 Hz, 2H), 7.33 (d, J=9.20 Hz, 2H), 7.28 (d, J=8.40 Hz, 2H), 6.84 (d, J=8.40 Hz, 2H), 5.31 (d, J=7.20 Hz, 1H), 3.82-3.76 (m, 5H), 3.10 (t, J=5.20 Hz, 4H), 2.37 (s, 3H), 1.67-1.45 (m, 3H), 0.84 (d, J=6.40 Hz, 3H), 0.65 (d, J=6.40 Hz, 3H)

(S)-tert-butyl 4-(5-(4-methyl-2-(4-methylphenylsulfonamido)pentanamido)pyridin-2-yl)piperazine-1-carboxylate

[0341] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.15 (s, 1H), 8.02 (d, J=2.80 Hz, 1H), 7.77 (d, J=8.40 Hz, 2H), 7.6 (dd, J=2.80, 9.20 Hz, 1H), 7.25 (d, J=8.40 Hz, 2H), 6.55 (d, J=9.20 Hz, 2H), 5.58 (d, J=8.00 Hz, 1H), 3.89-3.84 (m, 1H), 3.53-3.43 (m, 8H), 2.33 (s, 3H), 1.62-1.59 (m, 2H), 1.52-1.48 (m, 10H), 0.85 (d, J=5.60 Hz, 3H), 0.69 (d, J=6.00 Hz, 3H)

(S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(4-(pyrrolidin-1-yl)phenyl)pentanamide

[0342] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.76 (d, J=8.00 Hz, 2H), 7.71 (s, 1H), 7.23 (d, J=8.00 Hz, 2H), 7.08-7.04 (m, 2H), 6.43-6.39 (m, 2H), 5.47 (d, J=7.60 Hz, 1H), 3.85-3.79 (m, 1H), 3.22 (t, J=6.40 Hz, 4H), 2.43 (s, 3H), 2.03-1.96 (m, 4H), 1.64-1.47 (m, 3H), 0.86 (d, J=6.40 Hz, 3H), 0.74 (d, J=6.40 Hz, 3H)

(S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(2-morpholinoethyl)pentanamide

[0343] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.76-7.73 (m, 2H), 7.29 (d, J=8.00 Hz, 2H), 6.65 (t, J=4.80 Hz, 1H), 5.50 (d, J=7.20 Hz, 1H), 3.71-3.63 (m, 5H), 3.29-3.23 (m, 1H), 3.18-3.11 (m, 1H), 2.46-2.37 (m, 9H), 1.57-1.50 (m, 2H), 1.44-1.39 (m, 1H), 0.83 (d, J=6.40 Hz, 3H), 0.67 (d, J=6.00 Hz, 3H)

(S)—N-(4-methyl-1-morpholino-1-oxopentan-2-yl)-3-nitrobenzenesulfonamide

[0344] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.62 (t, J=2.00 Hz, 1H), 8.43-8.40 (m, 1H), 8.17-8.14 (m, 1H), 7.73 (t, J=8.00 Hz, 1H), 5.82 (d, J=10.0 Hz, 1H), 4.28-4.22 (m, 1H), 3.66-3.58 (m, 1H), 3.57-3.51 (m, 2H), 3.39-3.21 (m, 5H), 1.97-1.90 (m, 1H), 1.53-1.45 (m, 1H), 1.25-1.18 (m, 1H), 0.98 (d, J=6.80 Hz, 3H), 0.94 (d, J=6.40 Hz, 3H)

(S)-3-Amino-N-(4-methyl-1-morpholino-1-oxopentan-2-yl)benzenesulfonamide

[0345] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.23 (t, J=7.80 Hz, 1H), 7.14-7.09 (m, 2H), 6.80 (dd, J=1.40, 7.80 Hz, 1H), 4.11-4.02 (m, 3H), 3.61-3.53 (m, 2H), 3.44-3.35 (m, 3H), 3.29-3.20 (m, 3H), 1.97-1.93 (m, 1H), 1.51-1.41 (m, 1H), 1.19-1.13 (m, 1H), 0.95 (d, J=6.00 Hz, 3H), 0.91 (d, J=6.80 Hz, 3H)

(S)-2-(4-Fluorophenylsulfonamido)-4-methyl-N-(4-morpholinophenyl)pentanamide

[0346] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.98 (s, 1H), 7.91-7.87 (m, 2H), 7.22-7.19 (m, 2H), 7.12-7.07 (m, 2H), 6.80 (dd, J=2.20, 6.60 Hz, 2H), 5.74 (d, J=7.60 Hz, 1H), 3.85 (t, J=5.00 Hz, 4H), 3.09 (t, J=4.80 Hz, 4H), 1.63-1.57 (m, 2H), 1.53-1.48 (m, 1H), 0.86 (d, J=6.40 Hz, 3H), 0.73 (d, J=6.00 Hz, 3H)

(S)-2-(4-Bromophenylsulfonamido)-4-methyl-N-(4-morpholinophenyl)pentanamide

[0347] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.72 (d, J=8.40 Hz, 2H), 7.59 (d, J=8.40 Hz, 2H), 7.45 (s, 1H), 7.18 (d, J=9.20 Hz, 2H), 6.85 (d, J=8.80 Hz, 2H), 5.19 (d, J=8.00 Hz, 1H), 3.86 (t, J=4.60 Hz, 4H), 3.82-3.77 (m, 1H), 3.12 (t, J=5.00 Hz, 4H), 2.04-1.50 (m, 3H), 0.90 (d, J=6.40 Hz, 3H), 0.8 (d, J=5.60 Hz, 3H)

(S)-4-Methyl-N-(4-morpholinophenyl)-2-(4-(trifluoromethyl)phenylsulfonamido) pentanamide

[0348] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.99 (d, J=8.00 Hz, 2H), 7.68 (s, 1H), 7.66 (d, J=4.00 Hz, 2H), 7.10 (d, J=12.4 Hz, 2H), 6.79 (d, J=12.0 Hz, 2H), 5.70 (d, J=8.40 Hz, 1H), 3.92-3.98 (m, 1H), 3.85 (t, J=4.80 Hz, 4H), 3.09 (t, J=4.80 Hz, 4H), 1.67-1.54 (m, 3H), 0.89 (d, J=6.00 Hz, 3H), 0.79 (d, J=6.40 Hz, 3H)

(S)-4-Methyl-N-(4-morpholinophenyl)-2-(3-nitrophenylsulfonamido) pentanamide

[0349] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.70 (s, 1H), 8.26 (d, J=8.00 Hz, 1H), 8.0 (d, J=8.20 Hz, 1H), 7.95 (s, 1H), 7.61 (t, J=8.00 Hz, 1H), 7.12 (d, J=8.80 Hz, 2H), 6.73 (d, J=9.20 Hz, 2H)), 6.15 (d, J=8.80 Hz, 1H), 4.07-4.03 (m, 1H), 3.85 (t, J=4.60 Hz, 4H), 3.08 (t, J=4.60 Hz, 4H), 1.72-1.67 (m, 1H), 1.60-1.56 (m, 2H), 0.90 (d, J=6.40 Hz, 3H), 0.84 (d, J=6.40 Hz, 3H)

(S)-4-Methyl-N-(4-morpholinophenyl)-2-(naphthalene-1-sulfonamido)pentanamide

[0350] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.82 (d, J=8.40 Hz, 1H), 8.38 (dd, J=0.80, 7.60 Hz, 1H), 8.13 (s, 1H), 8.09 (d, J=8.00 Hz, 1H), 7.99 (d, J=8.00 Hz, 1H), 7.76-7.65 (m, 2H), 7.55 (t, J=7.80 Hz, 1H), 7.09-7.06 (m, 2H), 6.79-6.76 (m, 2H), 6.07 (d, J=7.20 Hz, 1H), 3.95-3.90 (m, 5H), 3.13 (t, J=4.60 Hz, 4H), 1.65-1.61 (m, 1H), 1.51-1.44 (m, 2H), 0.76 (d, J=6.00 Hz, 3H), 0.50 (d, J=6.80 Hz, 3H)

(S)-4-Methyl-N-(4-morpholinophenyl)-2-(naphthalene-2-sulfonamido)pentanamide

[0351] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.47 (s, 1H), 7.96 (s, 1H), 7.80-7.81 (m, 4H), 7.62-7.52 (m, 2H), 7.08-7.05 (m, 2H), 6.68-6.64 (m, 2H), 5.70 (d, J=7.60 Hz, 1H), 3.97-3.91 (m, 1H), 3.83 (t, J=4.80 Hz, 4H), 3.04 (t, J=4.80 Hz, 4H), 1.63-1.48 (m, 3H), 0.81 (d, J=6.40 Hz, 3H), 0.63 (d, J=5.60 Hz, 3H)

(S)-4-Methyl-N-(4-morpholinophenyl)-2-(phenylsulfonamido)pentanamide

[0352] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.89 (d, J=7.20 Hz, 2H), 7.75 (s, 1H), 7.56 (t, J=7.40 Hz, 1H), 7.49 (t, J=7.40 Hz, 2H), 7.24 (d, J=9.20 Hz, 2H), 6.82 (d, J=9.20 Hz, 2H), 5.20 (d, J=7.20 Hz, 2H)), 3.85 (t, J=4.80 Hz, 4H), 3.81-3.77 (m, 1H), 3.10 (t, J=4.80 Hz, 4H), 1.66-1.46 (m, 3H), 0.85 (d, J=6.00 Hz, 3H), 0.69 (d, J=6.00 Hz, 3H)

(S)-Benzyl 4-methyl-2-(3-(phenylsulfonyl)propanamido)pentanoate

[0353] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.50 (s, 1H), 7.42-7.31 (m, 7H), 6.88-6.84 (m, 2H), 5.01 (d, J=8.00 0 Hz, 1H), 4.27 (d, J=3.20 Hz, 2H), 3.86-3.81 (m, 5H), 3.12 (t, J=4.80 Hz, 4H), 1.74-1.60 (m, 2H), 1.54-1.47 (m, 1H), 0.93 (d, J=6.40 Hz, 3H), 0.90 (d, J=6.40 Hz, 3H)

(S)-2-(4-Methoxyphenylsulfonamido)-4-methyl-N-(4-morpholinophenyl)pentanamide

[0354] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.10 (s, 1H), 7.83-7.79 (m, 2H), 7.26-7.22 (m, 2H), 6.89-6.86 (m, 2H), 6.80-6.76 (m, 2H), 5.60 (d, J=7.60 Hz, 1H), 3.87-3.81 (m, 5H), 3.76 (s, 3H), 3.08 (t, J=5.40 Hz, 4H), 1.63-1.58 (m, 2H), 1.51-1.47 (m, 1H), 0.85 (d, J=6.00 Hz, 3H), 0.70 (d, J=5.60 Hz, 3H)

(S)-4-Methyl-N-(4-morpholinophenyl)-2-(thiophene-2-sulfonamido)pentanamide

[0355] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.73 (s, 1H), 7.65 (dd, J=1.20, 4.00 Hz, 1H), 7.58 (dd, J=1.20, 4.80 Hz, 1H), 7.30-7.27 (m, 2H), 7.05 (dd, J=3.60, 5.20 Hz, 1H), 6.85-6.81 (m, 2H), 5.34 (s, 1H), 3.91-3.84 (m, 5H), 3.11 (t, J=5.00 Hz, 4H), 1.72-1.51 (m, 3H), 0.89 (d, J=6.00 Hz, 3H), 0.79 (d, J=6.00 Hz, 3H)

(S)-4-Methyl-N-(4-morpholinophenyl)-2-(4-nitrophenylsulfonamido)pentanamide

[0356] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.23-8.21 (m, 2H), 8.03-8.00 (m, 2H), 7.12 (d, J=8.80 Hz, 2H), 6.79 (d, J=9.20 Hz, 2H), 5.49 (d, J=8.80 Hz, 1H), 3.91-3.84 (m, 5H), 3.10 (t, J=4.80 Hz, 4H), 1.76-1.70 (m, 1H), 1.61-1.58 (m, 3H), 0.93 (d, J=6.80 Hz, 3H), 0.87 (d, J=6.80 Hz, 3H)

(S)-2-(4-Isopropylphenylsulfonamido)-4-methyl-N-(4-morpholinophenyl)pentanamide

[0357] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.81-7.78 (m, 3H), 7.31 (d, J=8.40 Hz, 2H), 7.26-7.21 (m, 2H), 6.82-6.78 (m, 2H), 5.17 (d, J=6.40 Hz, 1H), 3.85 (t, J=4.00 Hz, 4H), 3.79-3.77 (m, 1H), 3.09 (t, J=4.80 Hz, 4H), 2.94-2.87 (m, 1H), 1.68-1.44 (m, 3H), 1.19 (d, J=6.80 Hz, 6H), 0.85 (d, J=6.00 Hz, 3H), 0.67 (d, J=6.00 Hz, 3H)

(S)-2-(Biphenyl-4-ylsulfonamido)-4-methyl-N-(4-morpholinophenyl)pentanamide

[0358] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.94 (d, J=8.20 Hz, 2H), 7.87 (brs, 1H), 7.59-7.64 (m, 2H), 7.37-7.49 (m, 5H), 7.15-7.20 (m, 2H), 6.72 (d, J=9.00 Hz, 2H), 5.48-5.60 (m, 1H), 3.87-3.95 (m, 1H), 3.79-3.85 (m, 4H), 2.98-3.05 (m, 4H), 1.62-1.69 (m, 2H), 1.51-1.60 (m, 1H), 0.88 (d, J=5.80 Hz, 3H), 0.76 (d, J=5.80 Hz, 3H)

(S)-4-(Benzyloxy)-N-(4-methyl-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)pentan-2-yl)benzenesulfonamide

[0359] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.76-7.73 (m, 2H), 7.41-7.32 (m, 5H), 7.03-6.99 (m, 2H), 5.55 (d, J=10.0 Hz, 1H), 5.11 (s, 2H), 4.22-4.17 (m, 1H), 3.78-3.39 (m, 13H), 3.22-3.06 (m, 3H), 1.97-1.90 (m, 1H), 1.48-1.33 (m, 2H), 0.92 (d, J=4.00 Hz, 3H), 0.89 (d, J=4.80 Hz, 3H)

(S)-4-Hydroxy-N-(4-methyl-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)pentan-2-yl)benzenesulfonamide

[0360] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.20 (s, 1H), 7.65 (d, J=8.80 Hz, 2H), 6.83 (d, J=8.80 Hz, 2H), 5.65 (d, J=9.60 Hz, 1H), 4.31-4.26 (m, 1H), 3.84-3.19 (m, 16H), 1.99-1.93 (m, 1H), 1.53-1.52 (m, 2H), 0.93 (t, J=6.20 Hz, 6H)

(S)-Benzyl 4-(N-(4-methyl-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)pentan-2-yl)sulfamoyl)benzoate

[0361] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.19-8.16 (m, 2H), 7.92-7.89 (m, 2H), 7.45-7.34 (m, 5H), 5.76 (d, J=9.20 Hz, 1H), 5.37 (s, 2H), 4.34-4.28 (m, 1H), 3.82-3.76 (m, 1H), 3.68-3.63 (m, 1H), 3.58-3.07 (m, 14H), 1.97-1.90 (m, 1H), 1.50-1.34 (m, 2H), 0.94 (d, J=6.40 Hz, 3H), 0.91 (d, J=6.80 Hz, 3H)

(S)-tert-Butyl 3-(4-methylphenylsulfonamido)-4-morpholino-4-oxobutanoate

[0362] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.72 (d, J=8.40 Hz, 2H), 7.31 (d, J=7.60 Hz, 2H), 5.89 (d, J=9.60 Hz, 1H), 4.55-4.498 (m, 1H), 3.62-3.28 (m, 8H), 2.55-2.40 (m, 4H), 1.41 (m, 9H)

(S)-4-Methyl-N-(1-morpholino-1-oxo-3-phenylpropan-2-yl)benzenesulfonamide

[0363] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.68 (d, J=4.80 Hz, 2H), 7.23-7.29 (m, 5H), 7.11-7.16 (m, 2H), 5.88 (d, J=9.60 Hz, 1H), 4.29-4.35 (m, 1H), 3.22-3.34 (m, 3H), 3.05-3.14 (m, 2H), 2.90-2.98 (m, 2H), 2.74-2.81 (m, 1H), 2.55-2.61 (m, 2H), 2.40 (s, 3H)

(S)—N-(3-hydroxy-1-morpholino-1-oxopropan-2-yl)-4-methylbenzenesulfonamide

[0364] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.74 (d, J=8.40 Hz, 2H), 7.32 (d, J=8.4 Hz, 2H), 6.00 (d, J=8.80 Hz, 1H), 4.19-4.24 (m, 1H), 3.52-3.68 (m, 4H), 3.34-3.49 (m, 6H), 2.82 (q, J=4.30 Hz, 1H), 2.44 (s, 3H)

(S)-4-Methyl-N-(3-methyl-1-morpholino-1-oxobutan-2-yl)benzenesulfonamide

[0365] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.69 (d, J=8.40 Hz, 2H), 7.29 (d, J=8.40 Hz, 2H), 5.66 (d, J=9.20 Hz, 1H), 3.81 (q, J=4.80 Hz, 1H), 3.51-3.58 (m, 2H), 3.24-3.35 (m, 5H), 3.10-3.17 (m, 1H), 2.42 (s, 3H), 1.76-1.84 (m, 1H), 1.02 (d, J=6.80 Hz, 3H), 0.88 (d, J=6.80 Hz, 3H)

(R)—N-(3-mercapto-1-morpholino-1-oxopropan-2-yl)-4-methylbenzenesulfonamide

[0366] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.76 (d, J=8.00 Hz, 2H), 7.33 (d, J=8.00 Hz, 2H), 5.95 (d, J=9.60 Hz, 1H), 4.48-4.53 (m, 1H), 3.54-3.63 (m, 2H), 3.30-3.45 (m, 6H), 2.95 (dd, J=7.00, 13.8 Hz, 1H), 2.84 (dd, J=6.20, 14.2 Hz, 1H), 2.44 (s, 3H)

(2S, 3S)-3-Hydroxy-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)butanamide

[0367] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 8.44 (s, 1H), 7.77 (d, J=7.20 Hz, 2H), 7.28-7.30 (m, 3H), 6.82 (d, J=8.80 Hz, 2H), 5.95 (d, J=7.20 Hz, 1H), 4.38-4.40 (m, 1H), 3.84 (t, J=4.60 Hz, 4H), 3.77 (dd, J=2.20, 6.60 Hz, 1H), 3.08-3.10 (m, 5H), 2.39 (s, 3H), 0.96 (d, J=6.40 Hz, 3H)

(2S,3S)-3-Methyl-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)pentanamide

[0368] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 9.57 (s, 1H), 7.84 (d, J=7.60 Hz, 1H), 7.61 (d, J=8.40 Hz, 2H), 7.18 (d, J=8.00 Hz, 2H), 7.11 (d, J=9.20 Hz, 2H), 6.80 (d, J=8.80 Hz, 2H), 3.71 (t, J=4.80 Hz, 4H), 3.57 (t, J=7.60 Hz, 1H), 3.00 (t, J=4.60 Hz, 4H), 2.20 (s, 3H), 1.50-1.63 (m, 2H), 1.08-1.12 (m, 1H), 0.76-0.79 (m, 6H)

(S)-2-(4-Methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide

[0369] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 9.63 (s, 1H), 8.00 (s, 1H) 7.66 (d, J=7.60 Hz, 2H), 7.23-7.29 (m, 4H), 6.84 (d, J=8.80 Hz, 2H), 3.87 (q, J=6.80 Hz, 1H), 3.71 (t, J=4.60 Hz, 4H), 3.01 (t, J=4.40 Hz, 4H), 2.29 (s, 3H), 1.12 (d, J=7.20 Hz, 3H)

(S)-2-(4-Methylphenylsulfonamido)-4-(methylthio)-N-(4-morpholinophenyl)butanamide

[0370] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.06 (s, 1H), 8.42 (s, 1H), 8.03 (d, J=8.00 Hz, 2H), 7.63 (d, J=8.40 Hz, 2H), 7.59 (d, J=9.20 Hz, 2H), 7.21 (d, J=8.80 Hz, 2H), 4.26-4.29 (m, 1H), 4.09 (t, J=4.40 Hz, 4H), 3.76 (s, 3H), 3.39 (t, J=4.60 Hz, 4H), 2.74-2.87 (m, 2H), 2.33 (s, 3H), 2.05-2.25 (m, 2H)

(S)-3-(1H-indol-2-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl) propanamide

[0371] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.75 (s, 1H), 9.64 (s, 1H), 8.05 (s, 1H), 7.50 (d, J=8.00 Hz, 2H), 7.39 (d, J=7.60 Hz, 1H), 7.27 (d, J=8.40 Hz, 1H), 7.18 (d, J=9.20 Hz, 2H), 7.09 (d, J=8.40 Hz, 2H), 7.06 (d, J=2.00 Hz, 1H), 7.02 (t, J=7.40 Hz, 1H), 6.91 (t, J=7.20 Hz, 1H), 6.81 (d, J=8.80 Hz, 2H), 3.99-4.06 (m, 1H), 3.71 (t, J=4.80 Hz, 4H), 2.99-3.05 (m, 5H), 2.79-2.85 (m, 1H), 2.18 (s, 3H)

(S)-3-(1-Methyl-1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl) propanamide

[0372] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.04 (s, 1H), 7.48 (d, J=8.20 Hz, 2H), 7.17-7.31 (m, 5H), 7.06 (d, J=8.20 Hz, 2H), 7.00 (dt, J=1.10, 7.20 Hz, 1H), 6.82 (d, J=9.00 Hz, 2H), 6.76 (s, 1H), 5.17 (d, J=6.20 Hz, 1H), 4.01 (q, J=6.20 Hz, 1H), 3.82-3.87 (m, 3H), 3.67 (s, 2H), 3.17 (dd, J=2.93, 6.46 Hz, 1H), 3.07-3.12 (m, 2H), 2.34 (s, 3H)

(S)-2-(4-Methylphenylsulfonamido)-N-(4-morpholinophenyl)-3-phenylpropanamide

[0373] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 9.64 (s, 1H), 8.11 (s, 1H), 7.48 (d, J=7.60 Hz, 2H), 7.12-7.20 (m, 9H), 6.81 (d, J=8.40 Hz, 2H), 4.03-4.05 (m, 1H), 3.71 (t, J=4.40 Hz, 4H), 3.01 (t, J=4.40 Hz, 4H), 2.85-2.90 (m, 1H), 2.70-2.73 (m, 1H), 2.24 (s, 3H)

(S)-Benzyl 4-methyl-2-(4-methylphenylsulfonamido)pentanoate

[0374] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.66-7.73 (m, 2H), 7.30-7.38 (m, 3H), 7.15-7.24 (m, 4H), 5.20 (d, J=10.1 Hz, 1H), 4.79-4.89 (m, 2H), 3.98 (ddd, J=6.20, 8.30, 10.0 Hz, 1H), 2.39 (s, 3H), 1.72-1.85 (m, 1H), 1.43-1.55 (m, 2H), 0.87 (dd, J=6.60, 7.80 Hz, 6H)

(S)-Benzyl 4-methyl-2-(4-methylbenzamido)pentanoate

[0375] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.69 (d, J=8.00 Hz, 2H), 7.39-7.32 (m, 5H), 7.24 (d, J=8.40 Hz, 2H), 6.48 (d, J=7.60 Hz, 1H), 5.20 (d, J=1.20 Hz, 2H), 4.93-4.87 (m, 1H), 2.40 (s, 3H), 1.80-1.62 (m, 3H), 0.97 (d, J=6.00 Hz, 3H), 0.95 (d, J=6.00 Hz, 3H)

(S)-Benzyl 2-(4-tert-butylbenzamido)-4-methylpentanoate

[0376] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.74-7.72 (m, 2H), 7.52-7.44 (m, 2H), 7.37-7.31 (m, 5H), 6.49 (d, J=8.40 Hz, 1H), 5.19 (s, 2H), 4.94-4.88 (m, 1H), 1.78-1.63 (m, 3H), 1.33 (s, 9H), 0.97 (d, J=6.00 Hz, 3H), 0.94 (d, J=5.60 Hz, 3H)

(S)-Benzyl 2-(benzo[d][1,3]dioxole-5-carboxamido)-4-methylpentanoate

[0377] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.71 (dd, J=2.00, 8.00 Hz, 1H), 7.51 (d, J=2.00 Hz, 1H), 7.38-7.33 (m, 5H), 6.86 (d, J=8.40 Hz, 1H), 6.06 (s, 2H), 5.16 (d, J=1.20 Hz, 2H), 3.56-3.52 (m, 1H), 1.78-1.73 (m, 1H), 1.63-1.56 (m, 1H), 1.48-1.41 (m, 1H), 0.93 (d, J=6.40 Hz, 3H), 0.91 (d, J=6.80 Hz, 3H)

(S)-Benzyl 2-(4-(tert-butoxycarbonylamino)benzamido)-4-methylpentanoate

[0378] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.75-7.72 (m, 2H), 7.43 (d, J=8.40 Hz, 2H), 7.39-7.31 (m, 5H), 6.61 (s, 1H), 6.43 (d, J=8.40 Hz, 1H), 5.19 (d, J=2.00 Hz, 2H), 4.92-4.86 (m, 1H), 1.78-1.62 (m, 3H), 0.97 (d, J=6.00 Hz, 3H), 0.95 (d, J=6.40 Hz, 3H)

(S)-Benzyl 4-methyl-2-(3-(phenylsulfonyl)propanamido)pentanoate

[0379] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.91-7.89 (m, 2H), 7.68-7.54 (m, 3H), 7.38-7.31 (m, 5H), 5.97 (d, J=8.00 Hz, 1H), 5.14 (s, 2H), 4.61-4.56 (m, 1H), 3.46-3.40 (m, 2H), 2.71-2.66 (m, 2H), 1.64-1.50 (m, 3H), 0.90 (d, J=5.60 Hz, 6H)

(S)—N-(4-(4-methoxyphenyl)thiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide

[0380] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 9.54 (brs, 1H), 7.75 (t, J=7.60 Hz, 4H), 7.26 (d, J=8.20 Hz, 2H), 6.99 (d, J=0.70 Hz, 1H), 6.95 (d, J=8.20 Hz, 2H), 5.19 (d, J=7.00 Hz, 1H), 3.91 (d, J=5.00 Hz, 1H), 3.84 (d, J=0.70 Hz, 3H), 2.32 (s, 3H), 1.53-1.63 (m, 2H), 1.43-1.51 (m, 1H), 0.84 (d, J=5.80 Hz, 3H), 0.68 (d, J=5.80 Hz, 3H)

(S)-1-(4-Methyl-1-morpholino-1-oxopentan-2-yl)-3-phenylurea

[0381] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.80 (s, 1H), 7.26-7.17 (m, 4H), 6.94-6.90 (m, 1H), 6.72 (d, J=8.80 Hz, 1H), 5.03-4.97 (m, 1H), 3.81-3.57 (m, 8H), 1.84-1.77 (m, 1H), 1.61-1.43 (m, 2H), 0.90 (d, J=3.60 Hz, 3H), 0.87 (d, J=7.20 Hz, 3H)

(S)-4-tert-Butyl-N-(4-methyl-1-morpholino-1-oxopentan-2-yl)benzamide

[0382] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 8.40 (s, 1H), 7.81 (d, J=8.00 Hz, 2H), 7.45 (d, J=8.80 Hz, 2H), 4.82-4.73 (m, 1H), 3.53-3.42 (m, 8H), 1.74-1.50 (m, 3H), 1.28 (s, 9H), 0.89 (d, J=6.80 Hz, 6H)

(S)—N-(4-Methyl-1-morpholino-1-oxopentan-2-yl)-3-(phenylsulfonyl)propanamide

[0383] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 8.30 (d, J=8.80 Hz, 1H), 7.88-7.86 (m, 2H), 7.75 (t, J=8.00 Hz, 1H), 7.65 (d, J=8.00 Hz, 2H), 4.66-4.61 (m, 1H), 3.52-3.25 (m, 10H), 2.46-2.42 (m, 2H), 1.52-1.46 (m, 1H), 1.38-1.33 (m, 2H), 0.82 (d, J=6.60 Hz, 6H)

(S)-4-tert-Butyl-N-(4-methyl-1-(4-morpholinophenylamino)-1-oxopentan-2-yl)benzamide

[0384] .sup.1H-NMR (400 MHz, MeOD) δ 7.81 (d, J=8.00 Hz, 2H), 7.51 (t, J=8.80 Hz, 2H), 7.45 (d, J=8.80 Hz, 2H), 6.94 (d, J=8.80 Hz, 2H), 4.85-4.81 (m, 1H), 3.82 (t, J=5.00 Hz, 3H), 3.10 (t, J=4.80 Hz, 3H), 1.82-1.62 (m, 3H), 1.28 (s, 9H), 1.03 (d, J=6.60 Hz, 6H)

(S)—N-(4-Methyl-1-(4-morpholinophenylamino)-1-oxopentan-2-yl)benzo[d][1,3]dioxole-5-carboxamide

[0385] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 9.84 (s, 1H), 8.35 (d, J=7.60 Hz, 1H), 7.52-7.44 (m, 4H), 6.97 (d, J=8.40 Hz, 1H), 6.87 (d, J=9.20 Hz, 2H), 6.08 (d, J=2.40 Hz, 2H), 4.60-4.54 (m, 1H), 3.71 (d, J=4.80 Hz, 4H), 3.02 (t, J=4.80 Hz, 4H), 1.74-1.50 (m, 3H), 0.92 (d, J=6.80 Hz, 3H), 0.89 (d, J=6.40 Hz, 3H)

(S)-4-Methyl-N-(4-morpholinophenyl)-2-(3-(phenylsulfonyl)propanamido)pentanamide

[0386] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.69-8.63 (m, 1H), 7.87 (d, J=7.20 Hz, 2H), 7.71-7.32 (m, 5H), 7.18-6.60 (m, 3H), 4.59-4.55 (m, 1H), 3.82 (t, J=5.00 Hz, 3H), 3.54-3.48 (m, 2H), 3.06 (t, J=4.80 Hz, 3H), 2.75-2.73 (m, 2H), 1.85-1.56 (m, 3H), 0.89 (d, J=6.2 Hz, 6H)

(S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide

[0387] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 12.44 (s, 1H), 10.78 (s, 1H), 8.51 (brs, 1H), 7.82-7.80 (d, J=8.50 Hz, 2H), 7.47-7.37 (m, 6H), 7.28-7.26 (d, J=8.00 Hz), 7.08-6.90 (m, 5H), 4.32 (brs, 1H), 3.79 (s, 3H), 3.33 (s, 2H), 3.11-3.07 (dd, J=14.5, 6.00 Hz, 1H), 2.90-2.85 (dd, J=14.0, 8.50 Hz, 1H)

(S)-3-(1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-2-(4-methylphenylsulfonamido)propanamide

[0388] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 12.3 (s, 1H), 10.7 (s, 1H), 8.24-8.22 (d, J=8.50 Hz, 1H), 7.95-7.93 (d, J=8.50 Hz, 1H), 7.50-7.48 (d, J=8.50 Hz, 2H), 7.15-7.09 (m, 4H), 6.97-6.95 (d, J=8.00 Hz, 1H), 6.74-6.58 (m, 6H), 4.01-3.96 (q, J=7.50 Hz, 1H), 3.47 (s, 3H), 2.79-2.74 (dd, J=14.2, 7.00 Hz, 1H), 2.56-2.51 (dd, J=14.5, 8.00 Hz, 1H), 1.86 (s, 3H)

(S)-3-(1H-indol-3-yl)-2-(2-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide

[0389] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.27 (s, 1H), 7.86-7.83 (m, 2H), 7.33-7.29 (m, 3H), 7.20-7.14 (m, 4H), 7.01-6.95 (m, 2H), 6.91 (d, J=2.40 Hz, 4H), 6.80-6.78 (m, 2H), 5.38 (d, J=5.60 Hz, 1H), 4.00-3.95 (m, 1H), 3.83 (t, J=4.60 Hz, 4H), 3.27-3.14 (m, 2H), 3.07 (t, J=5.00 Hz, 4H), 2.23 (s, 3H)

(S)-3-(1H-indol-3-yl)-2-(3-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide

[0390] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.76 (s, 1H), 9.70 (s, 1H), 8.11 (s, 1H), 7.45-7.39 (m, 3H), 7.28-7.19 (m, 5H), 7.06-7.00 (m, 2H), 6.93-6.89 (m, 1H), 6.81 (d, J=8.80 Hz, 2H), 4.09-4.07 (m, 1H), 3.71 (t, J=4.80 Hz, 4H), 3.05-2.99 (m, 5H), 2.85-2.79 (m, 1H), 2.14 (s, 3H)

(S)-2-(3,5-Dimethylphenylsulfonamido)-3-(1H-indol-3-yl)-N-(4 morpholinophenyl)propanamide

[0391] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.77 (s, 1H), 9.71 (s, 1H), 8.04 (s, 1H), 7.42 (d, J=8.00 Hz, 1H), 7.28-7.22 (m, 5H), 7.07-7.00 (m, 3H), 6.92 (t, J=7.40 Hz, 1H), 6.82 (d, J=9.20 Hz, 2H), 4.11-4.07 (m, 1H), 3.71 (t, J=4.80 Hz, 4H), 3.05-2.99 (m, 5H), 2.85-2.80 (m, 1H), 2.12 (s, 6H)

(S)-2-(4-Fluorophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propanamide

[0392] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.77 (d, J=2.00 Hz, 1H), 9.75 (s, 1H), 8.26 (s, 1H), 7.62-7.59 (m, 2H), 7.46 (d, J=8.00 Hz, 1H), 7.28-7.22 (m, 3H), 7.09-7.01 (m, 4H), 6.93 (t, J=7.40 Hz, 1H), 6.85-6.81 (m, 2H), 4.10 (s, 1H), 3.72 (t, J=4.80 Hz, 4H), 3.07-3.01 (m, 5H), 2.89-2.83 (m, 1H)

(S)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)-2-(4-(trifluoromethyl)phenylsulfon-amido)propanamide

[0393] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.77 (d, J=1.60 Hz, 1H), 9.79 (s, 1H), 8.55 (s, 1H), 7.72 (d, J=8.80 Hz, 2H), 7.57 (d, J=8.40 Hz, 2H), 4.47 (d, J=8.00 Hz, 1H), 7.25 (d, J=7.60 Hz, 1H), 7.19 (d, J=9.20 Hz, 2H), 7.11 (d, J=2.40 Hz, 1H), 7.02 (t, J=7.60 Hz, 1H), 6.92 (t, J=7.40 Hz, 1H), 6.81 (d, J=9.20 Hz, 2H), 4.14 (s, 1H), 3.72 (t, J=4.60 Hz, 4H), 3.08-2.99 (m, 5H), 2.92-2.86 (m, 1H)

(S)-3-(5-Hydroxy-1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide

[0394] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.45 (d, J=2.00 Hz, 1H), 9.63 (s, 1H), 8.54 (s, 1H), 8.02 (s, 1H), 7.53 (d, J=8.00 Hz, 2H), 7.18 (d, J=9.20 Hz, 2H), 7.11 (d, J=8.20 Hz, 2H), 7.07 (d, J=8.40 Hz, 1H), 6.97 (d, J=2.40 Hz, 1H), 6.81 (d, J=8.00 Hz, 2H), 6.77 (d, J=2.00 Hz, 1H), 6.57 (dd, J=2.00, 8.40 Hz, 1H), 4.09-4.06 (s, 1H), 3.72 (t, J=4.80 Hz, 4H), 3.01 (t, J=5.00 Hz, 4H), 2.96-2.91 (m, 1H), 2.76-2.70 (m, 1H), 2.23 (s, 3H)

(S)—N-(3-(1H-indol-3-yl)-1-morpholino-1-oxopropan-2-yl)-4-methylbenzenesulfonamide

[0395] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.19 (brs, 1H), 7.67-7.71 (m, 2H), 7.48 (d, J=7.83 Hz, 1H), 7.34 (d, J=8.22 Hz, 1H), 7.25 (d, J=7.83 Hz, 2H), 7.18 (dt, J=1.17, 7.63 Hz, 1H), 7.07-7.12 (m, 1H), 7.06 (d, J=1.96 Hz, 1H), 5.92 (d, J=9.78 Hz, 1H), 4.42 (dt, J=5.28, 9.88 Hz, 1H), 3.19-3.34 (m, 4H), 3.08-3.15 (m, 1H), 2.86-2.98 (m, 2H), 2.75 (m, 1H), 2.62-2.70 (m, 1H), 2.50-2.56 (m, 1H), 2.39 (s, 3H), 2.19 (m, 1H).

(S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(5-morpholinothiazol-2-yl)propan amide

[0396] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.20-8.24 (m, 1H), 7.54 (d, J=8.22 Hz, 2H), 7.20 (d, J=8.22 Hz, 2H), 7.01-7.10 (m, 3H), 6.91 (t, J=7.43 Hz, 1H), 6.86 (d, J=2.35 Hz, 1H), 6.48 (s, 1H), 6.17-6.23 (m, 1H), 4.27 (d, J=6.65 Hz, 1H), 3.78 (t, J=4.70 Hz, 4H), 3.16 (d, J=6.65 Hz, 2H), 2.87-2.99 (m, 4H), 2.25 (s, 3H)

(S)-2-(2,4-Dimethylphenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propanamide

[0397] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.75 (s, 1H), 9.58 (s, 1H), 7.98 (s, 1H), 7.54 (d, J=8.00 Hz, 1H), 7.38 (d, J=8.00 Hz, 1H), 7.28 (d, J=8.40 Hz, 1H), 7.19 (d, J=9.20 Hz, 2H), 7.08 (d, J=2.40 Hz, 1H), 7.02 (t, J=7.40 Hz, 1H), 6.90-6.81 (m, 5H), 4.05-4.03 (m, 1H), 3.72 (t, J=4.60 Hz, 4H), 3.04-3.00 (m, 5H), 2.90-2.85 (m, 1H), 2.39 (s, 3H), 2.15 (s, 3H)

3-(3-Ethoxy-2-(4-methylphenylsulfonamido)-3-oxopropyl)-1H-indole-5-carboxylic acid

[0398] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 12.37 (s, 1H), 11.17 (s, 1H), 8.37 (d, J=8.40 Hz, 1H), 8.01 (s, 1H), 7.68 (dd, J=1.40, 8.60 Hz, 1H), 7.48 (d, J=8.00 Hz, 1H), 7.35 (d, J=8.40 Hz, 1H), 7.20-7.08 (m, 3H), 3.96-3.90 (m, 1H), 3.08-3.06 (m, 1H), 2.94-2.88 (m, 1H), 2.31 (s, 1H), 0.86 (t, J=6.60 Hz, 3H)

(S)-2-(4-Methylphenylsulfonamido)-N-(4-morpholinophenyl)-3-(1-tosyl-1H-Imidazol-4-yl)propanamide

[0399] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.62 (s, 1H), 7.84 (s, 1H), 7.71 (t, J=8.40 Hz, 4H), 7.29-7.23 (m, 6H), 6.98 (s, 1H), 6.89 (d, J=6.40 Hz, 1H), 6.83 (dt, J=8.80 Hz, 2H), 3.99-3.97 (m, 1H), 3.85 (t, J=4.80 Hz, 4H), 3.10 (t, J=4.80 Hz, 4H), 3.01 (dd, J=5.60, 15.2 Hz, 1H), 2.61 (dd, J=4.80, 14.8 Hz, 1H), 2.40 (d, J=8.40 Hz, 6H)

(S)—N-(6-((2S,6R)-2,6-dimethylmorpholino)pyridin-3-yl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide

[0400] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.14 (brs, 1H), 8.00 (d, J=2.35 Hz, 1H), 7.86 (s, 1H), 7.62 (dd, J=2.74, 9.00 Hz, 1H), 7.49-7.53 (m, 2H), 7.33 (dd, J=3.91, 7.83 Hz, 2H), 7.20 (t, J=7.63 Hz, 1H), 7.08-7.12 (m, 2H), 7.02 (t, J=7.63 Hz, 1H), 6.96 (d, J=1.96 Hz, 1H), 6.57 (d, J=9.00 Hz, 1H), 5.11 (d, J=6.26 Hz, 1H), 4.05 (q, J=6.52 Hz, 1H), 3.97 (d, J=11.35 Hz, 2H), 3.67-3.77 (m, 2H), 3.12-3.28 (m, 2H), 2.45-2.53 (m, 2H), 2.36 (s, 3H), 1.27 (d, J=6.26 Hz, 6H)

(R)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide

[0401] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.80 (brs, 1H), 8.27 (s, 1H), 7.97 (s, 2H), 7.45-7.48 (m, 2H), 7.32 (d, J=7.83 Hz, 1H), 7.29 (d, J=3.52 Hz, 1H), 7.22 (s, 1H), 7.13 (t, J=7.43 Hz, 1H), 7.00 (d, J=8.22 Hz, 2H), 6.94 (s, 1H), 6.78-6.81 (m, J=9.00 Hz, 2H), 5.57 (d, J=6.65 Hz, 1H), 4.05 (d, J=6.65 Hz, 1H), 3.80-3.86 (m, 4H), 3.19 (dd, J=6.46, 13.50 Hz, 2H), 3.05-3.10 (m, 4H), 2.28 (s, 3H)

(S)—N-(3-fluoro-4-morpholinophenyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide

[0402] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.78 (s, 1H), 9.90 (s, 1H), 8.16 (brs, 1H), 7.51 (d, J=8.22 Hz, 2H), 7.40 (d, J=7.83 Hz, 1H), 7.29 (d, J=7.83 Hz, 1H), 7.22 (dd, J=2.15, 15.1 Hz, 1H), 7.09 (d, J=8.61 Hz, 3H), 7.04 (t, J=7.63 Hz, 1H), 6.89-6.99 (m, 3H), 4.06 (brs, 1H), 3.70-3.74 (m, 4H), 3.04 (dd, J=6.85, 14.3 Hz, 1H), 2.90-2.94 (m, 4H), 2.85 (dd, J=7.40, 14.4 Hz, 1H), 2.21 (s, 3H)

(S)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)-2-(4-nitrophenylsulfonamido)propanamide

[0403] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.71 (brs, 1H), 9.90 (s, 1H), 8.66 (brs, 1H), 7.84-7.90 (m, 2H), 7.56-7.61 (m, 2H), 7.48 (d, J=7.83 Hz, 1H), 7.29-7.35 (m, J=9.00 Hz, 2H), 7.12 (d, J=7.83 Hz, 1H), 7.05-7.08 (m, 1H), 6.87-6.96 (m, 2H), 6.81-6.86 (m, 2H), 4.13 (dd, J=5.28, 9.19 Hz, 1H), 3.70-3.75 (m, 4H), 2.98-3.05 (m, 5H), 2.88 (dd, J=9.78, 14.5 Hz, 1H)

(S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propanamide

[0404] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.77 (brs, 1H), 9.77 (s, 1H), 8.35 (brs, 1H), 7.40-7.48 (m, 5H), 7.28 (d, J=8.22 Hz, 1H), 7.19-7.24 (m, 2H), 7.07-7.11 (m, 1H), 7.04 (t, J=7.43 Hz, 1H), 6.91-6.96 (m, 1H), 6.81-6.86 (m, 2H), 4.10 (t, J=7.24 Hz, 1H), 3.69-3.75 (m, 4H), 3.00-3.08 (m, 5H), 2.86 (dd, J=8.41, 14.28 Hz, 1H)

(S)-3-(1H-indol-3-yl)-2-(4-methoxyphenylsulfonamido)-N-(4-morpholinophenyl)propanamide

[0405] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.78 (brs, 1H), 9.67 (s, 1H), 7.99 (brs, 1H), 7.54 (d, J=8.61 Hz, 2H), 7.41 (d, J=7.83 Hz, 1H), 7.28 (d, J=8.22 Hz, 1H), 7.22 (d, J=9.00 Hz, 2H), 7.07-7.10 (m, 1H), 7.03 (t, J=7.63 Hz, 1H), 6.90-6.95 (m, 1H), 6.81 (t, J=9.59 Hz, 4H), 4.06 (brs, 1H), 3.70-3.74 (m, 4H), 3.69 (s, 3H), 2.98-3.07 (m, 5H), 2.80-2.90 (m, 1H)

(S)-3-(1 Indol-3-yl)-2-(4-isopropylphenylsulfonamido)-N-(4 morpholinophenyl)propanamide

[0406] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.09 (brs, 1H), 8.03 (s, 1H), 7.81 (s, 1H), 7.58-7.62 (m, 2H), 7.33-7.38 (m, 2H), 7.18-7.25 (m, 5H), 7.05 (t, J=7.43 Hz, 1H), 6.97 (d, J=2.35 Hz, 1H), 6.80-6.85 (m, J=9.00 Hz, 2H), 5.11 (d, J=6.26 Hz, 1H), 4.08 (d, J=6.26 Hz, 1H), 3.83-3.89 (m, 4H), 3.34 (dd, J=6.06, 14.28 Hz, 1H), 3.09-3.16 (m, 5H), 1.25 (dd, J=2.35, 7.04 Hz, 6H)

(S)-3-(1H-indol-3-yl)-2-(4-isopropylphenylsulfonamido)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide

[0407] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.74 (d, J=8.40 Hz, 2H), 7.67 (d, J=7.60 Hz, 2H), 7.21 (t, J=6.80 Hz, 4H), 7.04 (s, 1H), 3.98-3.95 (m, 1H), 2.37 (s, 1H), 2.26 (m, 3H), 1.64-1.49 (m, 3H), 0.85 (d, J=6.40 Hz, 3H), 0.72 (d, J=6.40 Hz, 3H)

(S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-methylthiazol-2-yl)propanamide

[0408] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 12.13 (s, 1H), 10.83 (s, 1H), 8.26-8.24 (d, J=8.50 Hz, 1H), 7.45-7.44 (d, J=8.00 Hz, 2H), 7.39-7.38 (d, J=7.50 Hz, 1H), 7.29-7.27 (d, J=8.00 Hz, 1H), 7.06-7.02 (m, 4H), 6.91-6.89 (m, 1H), 6.72 (s, 1H), 4.27-4.22 (m, 1H), 3.07-3.03 (dd, J=14.2, 7.50 Hz, 1H), 2.86-2.81 (dd, J=14.2, 8.00 Hz, 1H), 2.24 (s, 3H), 2.22 (s, 3H)

(S)—N-(benzo[d]thiazol-2-yl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide

[0409] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 12.4 (s, 1H), 10.8 (s, 1H), 8.32 (m, 1H), 7.91 (m, 1H), 7.72 (m, 1H), 7.47-7.44 (m, 6H), 7.03-6.91 (m, 5H), 4.34 (brs, 1H), 3.11 (m, 1H), 2.91 (m, 1H), 2.08 (s, 3H)

(S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)propanoic acid

[0410] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 12.73 (brs, 1H), 10.80 (s, 1H), 8.41-8.39 (d, J=8.50 Hz, 1H), 7.51-7.49 (d, J=8.50 Hz, 2H), 7.42-7.40 (d, J=8.00 Hz, 2H), 7.32-7.29 (t, J=8.00 Hz, 2H), 7.08-7.03 (m, 2H), 6.94-6.91 (t, J=7.50 Hz, 1H), 3.94-3.89 (m, 1H), 3.10-3.08 (dd, J=14.5, 6.00 Hz, 1H), 2.89-2.84 (dd, J=14.0, 8.50 Hz, 1H)

(S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(5-morpholinothiazol-2-yl)pentanamide

[0411] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.71 (d, J=8.00 Hz, 2H), 7.16 (d, J=8.00 Hz, 2H), 6.95 (s, 1H), 6.35 (d, J=10.0 Hz, 1H), 4.14-4.06 (m, 1H), 3.86 (t, J=4.80 Hz, 4H), 3.13-3.07 (m, 4H), 2.29 (s, 3H), 1.75-1.70 (m, 1H), 1.60-1.53 (m, 1H), 1.46-1.41 (m, 1H), 0.81 (d, J=6.80 Hz, 6H)

(S)—N-(5-(4-methoxyphenyl)-1,3,4-thiadiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide

[0412] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 13.52 (s, 1H), 8.14 (d, J=8.80 Hz, 1H), 7.92-7.88 (m, 2H), 7.68 (d, J=8.40 Hz, 2H), 7.18 (d, J=8.40 Hz, 2H), 7.07-7.04 (m, 2H), 4.36-4.29 (m, 1H), 3.91 (s, 3H), 2.21 (s, 3H), 1.84-1.79 (m, 1H), 1.72-1.64 (m, 1H), 1.59-1.54 (m, 1H), 0.89 (d, J=6.40 Hz, 3H), 0.86 (d, J=6.80 Hz, 1H)

(S)—N-(5-(4-methoxyphenyl)isoxazol-3-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide

[0413] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 10.55 (s, 1H), 7.80-7.76 (m, 4H), 7.19-7.15 (m, 3H), 6.99 (d, J=9.20 Hz, 2H), 6.43 (d, J=9.20 Hz, 1H), 4.22-4.16 (m, 1H), 3.86 (s, 3H), 2.21 (s, 3H), 1.88-1.83 (m, 1H), 1.72-1.59 (m, 2H), 0.91 (d, J=6.80 Hz, 3H), 0.88 (d, J=6.40 Hz, 3H).

(S)—N-(3-(4-methoxyphenyl)isoxazol-5-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide

[0414] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 9.22 (s, 1H), 7.78 (d, J=8.40 Hz, 2H), 7.74-7.71 (m, 2H), 7.30 (d, J=8.00 Hz, 2H), 6.98-6.94 (m, 2H), 6.56 (s, 1H), 5.40 (d, J=7.20 Hz, 1H), 3.97-3.92 (m, 1H), 3.85 (s, 3H), 2.35 (s, 3H), 1.64-1.47 (m, 3H), 0.83 (d, J=6.40 Hz, 3H), 0.66 (d, J=5.60 Hz, 1H)

(S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(4-(4-(trifluoromethyl)phenyl)thiazol-2-yl)pentanamide

[0415] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 9.69 (s, 1H), 7.91 (d, J=8.40 Hz, 2H), 7.79 (d, J=8.40 Hz, 2H), 7.65 (d, J=8.40 Hz, 2H), 7.29-7.26 (m, 2H), 7.23 (s, 1H), 5.26 (d, J=6.80 Hz, 1H), 3.97-3.92 (m, 1H), 2.33 (s, 3H), 1.67-1.45 (m, 3H), 0.83 (d, J=6.40 Hz, 3H), 0.65 (d, J=6.40 Hz, 3H)

(S)—N-(4-(3,4-dimethoxyphenyl)thiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide

[0416] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 9.74 (s, 1H), 7.76 (d, J=7.60 Hz, 2H), 7.38-7.34 (m, 2H), 7.26 (d, J=6.80 Hz, 2H), 7.01 (s, 1H), 6.90 (d, J=8.00 Hz, 1H), 5.40 (d, J=6.80 Hz, 1H), 4.19-4.10 (m, 1H), 3.95 (s, 3H), 3.90 (s, 3H), 2.32 (s, 3H), 1.60-1.42 (m, 3H), 0.80 (d, J=6.00 Hz, 3H), 0.63 (d, J=5.60 Hz, 3H)

(S)—N-(4-(2-bromo-4-fluorophenyl)thiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide

[0417] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 9.62 (s, 1H), 7.78-7.75 (m, 4H), 7.26 (s, 1H), 7.10-7.05 (m, 3H), 5.31 (d, J=7.60 Hz, 1H), 3.95-3.92 (m, 1H), 2.32 (s, 3H), 1.64-1.46 (m, 3H), 0.82 (d, J=6.40 Hz, 3H), 0.66 (d, J=6.00 Hz, 3H).

(S)-4-(2-Aminothiazol-4-yl)phenyl 4-methyl-2-(4-methylphenylsulfonamido)pentanoate

[0418] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.79 (d, J=7.60 Hz, 2H), 7.67 (d, J=7.60 Hz, 2H), 7.29 (d, J=7.20 Hz, 2H), 6.68 (d, J=7.60 Hz, 2H), 6.65 (s, 1H), 5.53 (d, J=9.20 Hz, 1H), 5.27 (s, 2H), 4.16-4.11 (m, 1H), 2.41 (m, 3H), 1.90-1.87 (m, 1H), 1.63-1.60 (m, 1H), 1.27-1.24 (m, 1H), 0.94 (s, 6H)

(S)—N-(4-(4-fluorophenyl)thiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide

[0419] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 9.58 (s, 1H), 7.79-7.76 (m, 3H), 7.28-7.26 (m, 2H), 7.11-7.06 (m, 2H), 5.20 (d, J=6.80 Hz, 2H), 5.27 (s, 2H), 3.93-3.91 (m, 1H), 2.41 (m, 3H), 1.66-1.46 (m, 3H), 0.83 (d, J=6.40 Hz, 3H), 0.65 (d, J=6.40 Hz, 3H)

(S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(4-(4-(trifluoromethoxy)phenyl)thiazol-2-yl)pentanamide

[0420] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 9.60 (s, 1H), 7.83 (d, J=8.80 Hz, 2H), 7.79 (d, J=8.00 Hz, 2H), 7.29-7.23 (m, 4H), 7.13 (s, 1H), 5.21 (d, J=6.80 Hz, 1H), 3.93 (s, 1H), 2.33 (m, 3H), 1.65-1.48 (m, 3H), 0.83 (d, J=6.40 Hz, 3H), 0.64 (d, J=6.00 Hz, 3H)

(S)—N-(4-(4-hydroxyphenyl)thiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide

[0421] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.72 (d, J=8.00 Hz, 2H), 7.64 (d, J=8.80 Hz, 2H), 7.20 (d, J=8.00 Hz, 2H), 6.93 (s, 1H), 6.88 (d, J=8.40 Hz, 2H), 3.97-3.93 (m, 1H), 2.25 (s, 3H), 1.65-1.51 (m, 3H), 0.88 (d, J=6.40 Hz, 3H), 0.75 (d, J=6.00 Hz, 3H)

(S)-4-Methyl-2-(methylphenylsulfonamido)-N-(4p-tolylthiazol-2-yl)pentanamide

[0422] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.74 (d, J=8.40 Hz, 2H), 7.67 (d, J=7.60 Hz, 2H), 7.21 (t, J=6.80 Hz, 4H), 7.04 (s, 1H), 3.98-3.95 (m, 1H), 2.37 (s, 1H), 2.26 (m, 3H), 1.64-1.49 (m, 3H), 0.85 (d, J=6.40 Hz, 3H), 0.72 (d, J=6.40 Hz, 3H)

(S)—N-(4-(4((S)-1-methoxypropan-2-yloxy)phenyl)thiazol-2-yl)-4-methyl-2-(4-methylphenylsulfonamido)pentanamide

[0423] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 9.97 (s, 1H), 7.74 (d, J=8.40 Hz, 2H), 7.69 (d, J=8.80 Hz, 2H), 7.23 (d, J=8.00 Hz, 2H), 6.97 (s, 1H), 6.95 (d, J=9.20 Hz, 2H), 5.71 (d, J=7.60 Hz, 1H), 4.58-4.54 (m, 1H), 4.00-3.94 (m, 1H), 3.60-3.46 (m, 2H), 3.40 (s, 3H), 2.28 (s, 3H), 1.56-1.40 (m, 3H), 1.31 (d, J=6.00 Hz, 3H), 0.78 (d, J=6.00 Hz, 3H), 0.66 (d, J=5.60 Hz, 3H)

(S)-4-Methyl-2-(4-methylphenylsulfonamido)-N-(4-(4-morpholinophenyl)thiazol-2-yl)pentanamide

[0424] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.28 (dd, J=9.00, 11.4 Hz, 4H), 7.19 (d, J=8.40 Hz, 2H), 6.95 (t, J=4.60 Hz, 3H), 4.13-3.95 (m, 1H), 3.89 (t, J=4.80 Hz, 3H), 3.21 (t, J=5.00 Hz, 3H), 2.25 (s, 3H), 1.67-1.64 (m, 1H), 1.55-1.51 (m, 2H), 0.88 (d, J=6.80 Hz, 3H), 0.75 (d, J=6.40 Hz, 3H)

(S)-Methyl 4-(2-(4-methyl-2-(4-methylphenylsulfonamido)pentanamido)thiazol-4-yl)benzoate

[0425] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 10.05 (s, 1H), 8.18 (d, J=8.00 Hz, 2H), 7.93 (d, J=8.40 Hz, 2H), 7.76 (d, J=8.00 Hz, 2H), 7.26 (s, 1H), 7.20 (d, J=8.00 Hz, 2H), 5.63 (d, J=8.00 Hz, 1H), 4.12-4.09 (m, 1H), 3.99 (s, 3H), 2.24 (s, 3H), 1.65-1.52 (m, 1H), 0.86 (d, J=5.60 Hz, 3H), 0.74 (d, J=5.60 Hz, 3H)

(S)-4-(2-(4-Methylphenylsulfonamido)-3-(4-morpholinophenylamino)-3-oxopropyl)phenyl 4-methylbenzenesulfonate

[0426] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 9.62 (s, 1H), 9.18 (s, 1H), 8.05 (s, 1H), 7.49 (d, J=8.00 Hz, 2H), 7.15 (d, J=8.40 Hz, 4H), 6.93 (d, J=8.40 Hz, 2H), 6.83 (d, J=9.20 Hz, 2H), 6.58 (d, J=8.00 Hz, 2H), 3.95 (m, 1H), 3.72 (t, J=4.60 Hz, 4H), 3.02 (t, J=4.60 Hz, 4H), 2.78-2.58 (m, 2H), 2.25 (s, 3H)

(S)-2-(4-Bromophenylsulfonamido)-3-(1H-Imidazol-4-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide

[0427] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) 7.80-7.71 (d, J=9.00 Hz, 2H), 7.59 (s, 4H), 7.45-7.41 (d, J=15.0 Hz 2H), 6.98-6.96 (d, J=11.5 Hz, 2H), 6.75 (brs, 1H), 4.31-4.28 (t, J=7.50 Hz, 1H), 3.77 (s, 3H), 2.92-2.90 (dd, J.sub.1=14.0, 7.00 Hz, 1H), 2.77-2.73 (dd, J=14.0, 7.50 Hz, 1H)

(S)—N-methoxy-N,4-dimethyl-2-(4-methylphenylsulfonamido)pentanamide

[0428] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.72 (d, J=8.00 Hz, 2H), 7.27 (d, J=8.40 Hz, 2H), 5.40 (d, J=10.4 Hz, 1H), 4.28 (t, J=10.4 Hz, 1H), 3.56 (s, 3H), 2.92 (s, 3H), 2.40 (m, 3H), 1.92-1.89 (m, 1H), 1.45-1.39 (m, 3H), 1.31-1.24 (m, 1H), 0.91 (d, J=6.40 Hz, 6H)

(S)-3-(1H-indol-3-yl)-N-methoxy-N-methyl-2-(4-methylphenylsulfonamido)propanamide

[0429] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.00 (s, 1H), 7.54 (d, J=8.40 Hz, 2H), 7.44 (d, J=7.60 Hz, 1H), 7.31 (d, J=8.00 Hz, 1H), 7.16 (t, J=7.40 Hz, 1H), 7.11-7.03 (m, 4H), 5.46 (d, J=9.60 Hz, 1H), 4.61-4.55 (m, 1H), 3.45 (s, 3H), 3.17-3.12 (m, 1H), 3.05-3.00 (m, 1H), 2.95 (s, 3H), 2.34 (m, 3H)

(S)—N-(3-(1H-indol-3-yl)-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)propan-2-yl)-4-methylbenzenesulfonamide

[0430] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.25 (s, 1H), 7.60 (d, J=8.40 Hz, 2H), 7.47 (d, J=8.00 Hz, 1H), 7.29-7.26 (m, 1H), 7.14-7.02 (m, 5H), 5.86 (d, J=9.60 Hz, 1H), 4.66-4.60 (m, 1H), 3.67-3.63 (m, 1H), 3.58-3.36 (m, 13H), 3.25-2.97 (m, 4H)

(S)-2-(4-tert-Butylphenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propan amide

[0431] .sup.1H-NMR (400 MHz, CD.sub.3OD) δ 7.94 (s, 1H), 7.58-7.62 (m, 2H), 7.39 (d, J=7.83 Hz, 1H), 7.30-7.34 (m, 2H), 7.25 (d, J=7.83 Hz, 1H), 6.99-7.04 (m, 4H), 6.90 (s, 1H), 6.77 (d, J=9.00 Hz, 2H), 4.06 (s, 1H), 3.75-3.79 (m, 4H), 3.12-3.20 (m, 1H), 2.98-3.05 (m, 5H), 1.18 (s, 9H)

(S)-2-(4-Bromophenylsulfonamido)-N-(4-(2-chlorophenyl)thiazol-2-yl)-3-(1H-indol-3-yl)propanamide

[0432] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 2.89-2.93 (dd, J=14.67, 8.80 Hz, 1H), 3.10-3.14 (dd, J=14.18, 6.35 Hz, 1H), 4.34 (brs, 1H), 6.91-6.94 (t, J=7.33 Hz, 1H), 7.04-7.07 (t, J=7.82 Hz, 1H), 7.11 (s, 1H), 7.28-7.30 (d, J=8.31 Hz, 1H), 7.37-7.45 (m, 6H), 7.47-7.49 (d, J=7.82 Hz, 1H), 7.55-7.57 (d, J=7.82 Hz, 1H), 7.60 (s, 1H), 7.81-7.83 (m, 1H), 8.55 (brs, 1H), 10.80 (brs, 1H), 12.53 (brs, 1H)

(S)-2-(4-Bromophenylsulfonamido)-N-(4-(2,4-dimethoxyphenyl)thiazol-2-yl)-3-(1H-indol-3-yl)propanamide

[0433] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 2.85-2.90 (dd, J=14.18, 8.80 Hz, 1H), 3.08-3.12 (dd, J=14.67, 6.35 Hz, 1H), 3.80 (s, 3H), 3.90 (s, 3H), 4.32-4.34 (d, J=6.35 Hz, 1H), 6.61-6.63 (d, J=8.80 Hz, 1H), 6.66 (s, 1H), 6.90-6.93 (t, J=7.33 Hz, 1H), 7.03-7.06 (t, J=7.33 Hz, 1H), 7.08 (s, 1H), 7.26-7.28 (d, J=7.82 Hz, 1H), 7.36-7.40 (m, 4H), 7.47-7.48 (m, 2H), 7.96-7.98 (d, J=8.80 Hz, 1H), 8.51-8.52 (d, J=6.84 Hz, 1H), 10.78 (s, 1H), 12.39 (s, 1H)

(S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(thiazol-2-yl)propanamide

[0434] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 12.34 (s, 1H), 10.80 (s, 1H), 8.53 (s, 1H), 7.48-7.45 (m, 2H), 7.40-7.36 (m, 4H), 7.30-7.27 (m, 1H), 7.23-7.20 (m, 1H), 7.10-7.02 (m, 2H), 6.95-6.90 (m, 1H), 4.33 (brs, 1H), 3.12-3.07 (m, 1H), 2.92-2.86 (m, 1H)

(S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(5-methylthiazol-2-yl)propanamide

[0435] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 12.10 (s, 1H), 10.80 (s, 1H), 8.50-8.45 (d, J=8.00 Hz, 1H), 7.46-7.45 (d, J=7.50 Hz, 1H), 7.41-7.36 (m, 4H), 7.29-7.27 (d, J=8.00 Hz, 1H), 7.11-7.03 (m, 3H), 6.93-6.90 (t, J=7.00 Hz, 1H), 4.32-4.27 (m, 1H), 3.08-3.04 (dd, J=14.20, 6.50 Hz, 1H), 2.89-2.85 (dd, J=14.20, 8.50 Hz, 1H), 2.52 (s, 3H)

(S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-methylthiazol-2-yl)propanamide

[0436] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 12.2 (s, 1H), 10.8 (s, 1H), 8.53-8.52 (d, J=8.50 Hz, 1H), 7.45-7.44 (d, J=8.00 Hz, 1H), 7.39 (m, 4H), 7.28-7.27 (d, J=8.00 Hz, 1H), 7.07-7.02 (m, 2H), 6.92-6.90 (t, J=7.00 Hz, 1H), 6.75 (s, 1H), 4.29-4.25 (m, 1H), 3.09-3.05 (dd, J=14.2, 6.00 Hz, 1H), 2.89-2.85 (dd, J=14.7, 8.00 Hz, 1H), 2.52 (s, 3H)

(S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(5-methylthiazol-2-yl)propanamide

[0437] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 12.01 (s, 1H), 10.79 (s, 1H), 8.25 (d, J=8.00 Hz, 1H), 7.46-7.44 (m, 2H), 7.40-7.39 (d, J=7.50 Hz, 1H), 7.29-7.27 (d, J=8.00 Hz, 1H), 7.10-7.02 (m, 5H), 6.93-6.90 (m, 1H), 4.28-4.26 (m, 1H), 3.04-3.03 (dd, J=14.2, 7.00 Hz, 1H), 2.86-2.84 (dd, J=14.2, 7.00 Hz, 1H), 2.32 (s, 3H), 2.22 (s, 3H)

(S)-Methyl 4-(N-(3-(1H-indol-3-yl)-1-(4-morpholinophenylamino)-1-oxopropan-2-yl)sulfamoyl)benzoate

[0438] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.74 (s, 1H), 9.77 (s, 1H), 8.44 (s, 1H), 7.74 (d, J=8.40 Hz, 2H), 7.62 (d, J=8.00 Hz, 2H), 7.44 (d, J=7.20 Hz, 1H), 7.22 (t, J=8.40 Hz, 3H), 7.08 (d, J=2.00 Hz, 1H), 6.99 (d, J=7.40 Hz, 1H), 6.90 (t, J=7.20 Hz, 1H), 6.81 (d, J=9.20 Hz, 2H), 4.13-4.09 (m, 1H), 3.72 (t, J=4.60 Hz, 4H), 3.05-3.00 (m, 5H), 2.89-2.83 (m, 1H)

(S)-Ethyl 4-(N-(3-(1H-indol-3-yl)-1-(4-morpholinophenylamino)-1-oxopropan-2-yl)sulfamoyl)benzoate

[0439] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.74 (s, 1H), 9.76 (s, 1H), 7.73 (d, J=8.80 Hz, 2H), 7.62 (d, J=8.40 Hz, 2H), 7.44 (d, J=7.60 Hz, 1H), 7.23-7.20 (m, 3H), 7.09 (d, J=2.40 Hz, 1H), 7.00-6.81 (m, 2H), 6.81 (d, J=9.20 Hz, 2H), 4.31 (d, J=7.10 Hz, 2H), 4.12-4.09 (m, 1H), 3.72 (t, J=4.60 Hz, 4H), 3.05-3.00 (m, 5H), 2.89-2.83 (m, 1H), 1.34 (t, J=7.00 Hz, 3H)

(S)-3-(4-Benzoylphenyl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide

[0440] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 9.75 (s, 1H), 7.68 (d, J=7.20 Hz, 3H), 7.57 (t, J=5.80 Hz, 4H), 7.47 (d, J=8.00 Hz, 2H), 7.33 (d, J=8.00 Hz, 2H), 7.20 (d, J=8.80 Hz, 2H), 7.12 (d, J=7.60 Hz, 2H), 6.85 (d, J=8.80 Hz, 2H), 4.31 (d, J=7.10 Hz, 2H), 4.12-4.09 (m, 1H), 3.72 (t, J=4.40 Hz, 4H), 3.04-2.95 (m, 5H), 2.20 (s, 3H)

(S)-4-(N-(3-(1H-indol-3-yl)-1-(4-morpholinophenylamino)-1-oxopropan-2-yl)sulfamoyl)-N-methylbenzamide

[0441] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.75 (s, 1H), 9.72 (s, 1H), 8.44 (d, J=4.00 Hz, 1H), 8.22 (s, 1H), 7.75 (d, J=8.40 Hz, 2H), 7.67 (d, J=8.00 Hz, 2H), 7.42 (d, J=7.60 Hz, 1H), 7.26 (d, J=8.00 Hz, 1H), 7.18 (d, J=9.20 Hz, 2H), 7.07 (d, J=1.60 Hz, 1H), 7.01 (t, J=7.60 Hz, 1H), 6.92 (t, J=7.60 Hz, 1H), 6.79 (d, J=8.80 Hz, 2H), 4.15-4.11 (m, 1H), 3.72 (t, J=4.80 Hz, 4H), 3.08-2.99 (m, 5H), 2.88-2.82 (m, 3H), 2.78 (d, J=4.40 Hz, 3H)

(S)-2-(4-Methylphenylsulfonamido)-N-(4-morpholinophenyl)-3-(naphthalen-2-yl)propanamide

[0442] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 9.64 (s, 1H), 8.27 (s, 1H), 7.89-7.84 (m, 2H), 7.75 (t, J=4.60 Hz, 1H), 7.50-7.46 (m, 4H), 7.33 (d, J=4.20 Hz, 2H), 7.17 (d, J=8.80 Hz, 2H), 7.09 (d, J=8.40 Hz, 2H), 7.82 (d, J=9.20 Hz, 2H), 4.17-4.14 (m, 1H), 3.72 (t, J=4.60 Hz, 4H), 3.40-3.34 (m, 1H), 3.18-3.13 (m, 1H), 3.02 (t, J=5.00 Hz, 4H), 2.24 (s, 3H)

(S)-tert-Butyl 3-(1H-Indol-3-yl)-1-(4-morpholinophenylamino)-1-oxopropan-2-ylcarbamate

[0443] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.80 (s, 1H), 9.80 (s, 1H), 7.64 (d, J=8.00 Hz, 1H), 7.45 (d, J=9.20 Hz, 2H), 7.32 (d, J=8.40 Hz, 1H), 7.15 (s, 1H), 7.05 (t, J=7.40 Hz, 1H), 6.97 (t, J=7.20 Hz, 2H), 6.90-6.84 (m, 3H), 4.34-4.33 (m, 1H), 3.73 (t, J=4.80 Hz, 4H), 3.13-2.95 (m, 6H), 1.32 (s, 9H)

(S)-3-(1-Indol-3-yl)-2-(4-methylphenylsulfonamido)propanoic acid

[0444] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ10.77 (s, 1H), 8.12 (d, J=8.00 Hz, 1H), 7.45 (d, J=4.00 Hz, 2H), 7.25 (t, J=12.00 Hz, 2H), 7.12 (d, J=16.40 Hz, 2H), 6.96-7.01 (m, 2H), 6.88 (t, J=11.80 Hz, 1H), 3.86 (m, 1H), 3.03 (m, 1H), 2.83 (m, 1H), 2.30 (s, 3H)

(S)-tert-Butyl 4-(4-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)-3-methoxyphenyl)piperazine-1-carboxylate

[0445] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.42 (s, 1H), 8.36 (s, 1H), 8.11 (d, J=8.80 Hz, 1H), 7.48 (d, J=8.00 Hz, 2H), 7.33 (d, J=8.00 Hz, 1H), 7.28 (d, J=8.40 Hz, 1H), 7.14 (t, J=7.60 Hz, 1H), 7.02-6.96 (m, 2H), 6.92 (d, J=2.40 Hz, 1H), 6.45 (dd, J=2.40, 9.20 Hz, 1H), 6.41 (d, J=2.40 Hz, 1H), 5.25 (d, J=6.40 Hz, 1H), 4.14-4.05 (m, 1H), 3.57 (t, J=5.20 Hz, 4H), 3.20 (d, J=6.80 Hz, 2H), 3.05 (t, J=4.80 Hz, 4H), 2.28 (s, 6H), 1.48 (s, 9H)

(S)-3-(1H-indol-3-yl)-N-(2-methoxy-4-(piperazin-1-yl)phenyl)-2-(4-methylphenylsulfonamido)propanamide

[0446] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.69 (s, 1H), 8.97 (s, 1H), 7.50 (d, J=9.20 Hz, 1H), 7.40 (d, J=7.60 Hz, 2H), 7.35 (d, J=8.00 Hz, 1H), 7.26 (d, J=7.60 Hz, 1H), 7.08 (d, J=2.00 Hz, 1H), 7.03-7.00 (m, 3H), 6.90 (d, J=7.40 Hz, 1H), 6.56 (d, J=2.40 Hz, 1H), 6.38 (dd, J=2.60, 8.60 Hz, 1H), 4.12-4.09 (m, 2H), 3.77 (s, 3H), 3.10-3.05 (m, 1H), 3.01 (t, J=4.80 Hz, 4H), 2.85-2.79 (m, 5H), 2.24 (s, 3H)

(S)-tert-Butyl 4-(4-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)phenyl)piperazine-1-carboxylate

[0447] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.28 (s, 1H), 8.02 (s, 1H), 7.46 (d, J=8.40 Hz, 2H), 7.30 (d, J=8.80 Hz, 2H), 7.24 (d, J=7.20 Hz, 2H), 7.16 (t, J=7.20 Hz, 1H), 7.04 (d, J=8.00 Hz, 2H), 6.98 (t, J=7.40 Hz, 1H), 6.93 (d, J=2.40 Hz, 1H), 6.82 (d, J=9.20 Hz, 2H), 5.19 (d, J=5.60 Hz, 1H), 4.01-4.00 (m, 1H), 3.56 (t, J=5.20 Hz, 4H), 3.18 (d, J=6.00 Hz, 2H), 3.05 (t, J=4.80 Hz, 4H), 2.31 (s, 3H), 1.48 (s, 9H)

(S)-3-(1H-indol-3-yl)-N-(2-methoxy-4-morpholinophenyl)-2-(4-methylphenylsulfonamido)propanamide

[0448] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.37 (s, 1H), 8.13 (d, J=8.80 Hz, 1H), 8.02 (s, 1H), 7.53 (d, J=8.00 Hz, 2H), 7.36 (d, J=8.00 Hz, 1H), 7.32 (d, J=8.40 Hz, 1H), 7.18 (t, J=7.60 Hz, 1H), 7.08 (d, J=8.40 Hz, 2H), 7.02 (t, J=7.00 Hz, 1H), 6.96 (d, J=2.40 Hz, 1H), 6.47 (dd, J=2.40, 8.80 Hz, 1H), 6.41 (d, J=2.40 Hz, 1H), 5.08 (d, J=6.40 Hz, 1H), 4.14-4.05 (m, 1H), 3.86 (t, J=4.60 Hz, 4H), 3.73 (s, 3H), 3.29-3.14 (m, 2H), 3.11 (t, J=4.80 Hz, 4H), 2.32 (s, 3H)

(S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-(piperazin-1-yl)phenyl)propanamide

[0449] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.76 (s, 1H), 9.63 (s, 1H), 7.51 (d, J=8.40 Hz, 2H), 7.40 (d, J=7.60 Hz, 1H), 7.28 (d, J=8.40 Hz, 1H), 7.17 (d, J=8.80 Hz, 2H), 7.10-7.01 (m, 4H), 6.92 (t, J=7.20 Hz, 1H), 6.79 (d, J=9.20 Hz, 2H), 4.08-4.05 (m, 2H), 3.05-3.00 (m, 1H), 2.95 (t, J=4.80 Hz, 4H), 2.85-2.79 (m, 5H), 2.23 (s, 3H)

(S)-3-(1-Formyl-1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide

[0450] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 9.86 (s, 1H), 9.14 (s, 1H), 8.23 (s, 1H), 8.15 (s, 1H), 7.60-7.43 (m, 2H), 7.37-7.28 (m, 6H), 6.95 (d, J=8.00 Hz, 2H), 6.88 (d, J=8.40 Hz, 2H), 4.13 (m, 2H), 3.73 (t, J=4.60 Hz, 3H), 3.05-2.96 (m, 5H), 2.89-2.83 (m, 1H), 2.20 (s, 3H)

(S)-3-(1H-indol-3-yl)-N-(3-(4-methoxyphenyl)isoxazol-5-yl)-2-(4-methylphenylsulfonamido)propanamide

[0451] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 9.42 (s, 1H), 8.28 (d, J=1.60 Hz, 1H), 7.73-7.70 (m, 2H), 7.42 (d, J=8.40 Hz, 2H), 7.22 (t, J=7.60 Hz, 1H), 7.12 (t, J=7.60 Hz, 1H), 6.97-6.90 (m, 6H), 6.65 (s, 1H), 5.39 (d, J=6.00 Hz, 1H), 4.15-4.09 (m, 1H), 3.83 (s, 3H), 3.26-3.08 (m, 2H), 2.25 (s, 3H)

(S)-Benzyl 3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanoate

[0452] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.06 (brs, 1H), 7.57 (d, J=8.20 Hz, 2H), 7.42 (d, J=8.20 Hz, 1H), 7.25-7.33 (m, 4H), 7.08-7.18 (m, 3H), 6.99-7.07 (m, 3H), 6.84 (d, J=2.30 Hz, 1H), 5.24 (d, J=9.00 Hz, 1H), 4.74-4.83 (m, 2H), 4.29 (td, J=5.60, 9.00 Hz, 1H), 3.17-3.27 (m, 2H), 2.34 (s, 3H)

(S)-Benzyl 3-(1H-indol-3-yl)-2-(4-methylbenzamido)propanoate

[0453] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.95 (brs, 1H), 7.52-7.60 (m, 3H), 7.33-7.38 (m, 3H), 7.27-7.32 (m, 2H), 7.16-7.21 (m, 3H), 7.06 (t, J=7.43 Hz, 1H), 6.75 (d, J=2.35 Hz, 1H), 6.64 (d, J=7.83 Hz, 1H), 5.17-5.23 (m, 1H), 5.14 (d, J=7.04 Hz, 2H), 3.44 (d, J=5.09 Hz, 2H), 2.37 (s, 3H)

(S)—N-(3-(1 Indol-3-yl)-1-(4-morpholinophenylamino)-1-oxopropan-2-yl)-4-methylbenzamide

[0454] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.10 (brs, 1H), 7.84 (d, J=7.83 Hz, 1H), 7.64 (d, J=8.22 Hz, 2H), 7.38 (d, J=8.22 Hz, 1H), 7.15-7.24 (m, 5H), 7.14 (d, J=2.35 Hz, 1H), 7.03 (d, J=7.43 Hz, 1H), 6.78-6.82 (m, 2H), 5.06 (dt, J=5.09, 7.83 Hz, 1H), 3.82-3.86 (m, 4H), 3.57 (dd, J=5.09, 14.48, 4H)

(S)-3-Hydroxy-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide

[0455] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.39 (s, 1H), 7.79 (d, J=8.40 Hz, 2H), 7.33-7.38 (m, 4H), 6.87 (d, J=9.20 Hz, 2H), 5.69 (s, 1H), 4.11 (d, J=10.40 Hz, 1H), 3.85-3.87 (m, 5H), 3.49-3.50 (m, 1H), 3.36-3.39 (m, 1H), 3.12 (t, J=5.00 Hz, 4H), 2.43 (s, 3H), 2.30 (s, 1H)

(S)-3-Methyl-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)butanamide

[0456] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 9.56 (s, 1H), 7.81 (s, 1H), 7.62 (d, J=8.00 Hz, 2H), 7.20 (d, J=8.40 Hz, 2H), 7.13 (d, J=8.80 Hz, 2H), 6.81 (d, J=8.80 Hz, 2H), 3.71 (t, J=4.80 Hz, 4H), 3.53 (d, J=7.60 Hz, 1H), 3.00 (t, J=4.60 Hz, 4H), 1.81-1.86 (m, 1H), 0.82 (q, J=6.10 Hz, 6H)

(S)-1-(3-(1H-indol-3-yl)-1-morpholino-1-oxopropan-2-yl)-3-phenylurea

[0457] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.90 (s, 1H), 8.72 (s, 1H), 7.53 (d, J=7.60 Hz, 1H), 7.36 (t, J=8.20 Hz, 3H), 7.22-7.17 (m, 3H), 7.06 (d, J=3.40 Hz, 1H), 7.00-6.89 (m, 2H), 6.59 (d, J=8.00 Hz, 1H), 4.96 (d, J=6.00 Hz, 1H), 3.45-3.42 (m, 2H), 3.26-3.04 (m, 8H)

(S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(6-morpholinopyridin-3-yl)propanamide

[0458] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.78 (s, 1H), 9.71 (s, 1H), 8.12 (s, 1H), 8.00 (d, J=2.40 Hz, 1H), 7.53 (d, J=8.00 Hz, 2H), 7.45 (dd, J=2.40, 9.20 Hz, 1H), 7.40 (d, J=8.00 Hz, 1H), 7.29 (d, J=7.60 Hz, 1H), 7.12 (d, J=7.60 Hz, 2H), 7.08 (d, J=2.00 Hz, 1H), 7.04 (t, J=7.40 Hz, 1H), 6.92 (t, J=7.40 Hz, 1H), 6.74 (d, J=9.20 Hz, 1H), 4.06 (s, 1H), 3.68 (t, J=4.80 Hz, 4H), 3.34-3.33 (m, 4H), 3.07-3.01 (m, 1H), 2.88-2.82 (m, 1H)

(S)-3-(1H-Indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(2-morpholinopyrimidin-5-yl)propanamide

[0459] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.80 (s, 1H), 9.75 (s, 1H), 8.19 (s, 1H), 8.15 (s, 2H), 7.54 (d, J=8.40 Hz, 2H), 7.40 (d, J=8.00 Hz, 1H), 7.30 (d, J=8.00 Hz, 1H), 7.15 (d, J=8.40 Hz, 1H), 7.09 (s, 1H), 7.04 (t, J=7.40 Hz, 1H), 6.93 (t, J=7.40 Hz, 1H), 4.04 (m, 1H), 3.62-3.61 (m, 8H), 3.08-3.02 (m, 1H), 2.91-2.85 (m, 1H), 2.23 (s, 3H)

(S)-2-(4-Cyanophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propanamide

[0460] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.72 (s, 1H), 9.85 (s, 1H), 8.57 (s, 1H), 7.57 (s, 4H), 7.48 (d, J=7.60 Hz, 1H), 7.29-7.23 (m, 3H), 7.07-7.01 (m, 2H), 6.93 (t, J=7.20 Hz, 1H), 6.86 (d, J=8.80 Hz, 2H), 4.12 (s, 1H), 3.73 (s, 4H), 3.04-3.00 (m, 3H), 2.90-2.84 (m, 1H)

(S)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)-2-(6-(trifluoromethyl)pyridine-3-sulfonamido)propanamide

[0461] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.76 (s, 1H), 9.92 (s, 1H), 8.87 (s, 1H), 8.81 (s, 1H), 8.0 (d, J=8.40 Hz, 1H), 7.60 (d, J=8.00 Hz, 1H), 7.52 (d, J=7.60 Hz, 1H), 7.22-7.19 (m, 3H), 7.12 (d, J=1.60 Hz, 1H), 7.01 (d, J=7.40 Hz, 1H), 6.92 (d, J=7.40 Hz, 1H), 6.82 (d, J=9.20 Hz, 2H), 4.21 (m, 1H), 3.73 (t, J=4.40 Hz, 4H), 3.08-2.90 (m, 6H)

(S)-Methyl 4-(methylphenylsulfonamido)-5-(4-morpholinophenylamino)-5-oxopentanoate

[0462] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.16 (s, 1H), 7.74 (d, J=8.40 Hz, 2H), 7.27-7.25 (m, 4H), 6.83 (d, J=8.80 Hz, 2H), 6.21 (d, J=7.20 Hz, 1H), 3.9-3.84 (m, 5H), 3.69 (s, 3H), 3.10 (t, J=4.60 Hz, 4H), 2.58-2.50 (m, 1H), 2.36 (s, 3H), 2.32-2.25 (m, 1H), 2.05-1.93 (m, 2H)

(S)-3-(1H-benzo[d]imidazol-1-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide

[0463] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.97 (s, 1H), 7.68 (s, 1H), 7.57 (d, J=7.60 Hz, 2H), 7.38 (d, J=8.00 Hz, 1H), 7.27 (d, J=8.00 Hz, 1H), 7.12-7.00 (m, 6H), 6.72 (d, J=8.80 Hz, 2H), 4.49 (s, 2H), 4.44-4.43 (m, 1H), 3.80 (t, J=4.60 Hz, 4H), 3.03 (t, J=4.60 Hz, 4H), 2.24 (s, 3H)

(R)-3-(2,3-dioxo-3,4-dihydroquinoxalin-1(2H)-yl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide

[0464] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.48 (d, J=8.80 Hz, 2H), 7.43 (d, J=7.60 Hz, 2H), 7.37 (d, J=8.00 Hz, 1H), 7.32 (s, 1H), 7.27-7.20 (m, 2H), 7.07 (d, J=7.20 Hz, 1H), 6.91 (t, J=6.60 Hz, 4H), 4.75-4.68 (m, 1H), 4.32 (d, J=12.4 Hz, 2H), 3.87 (s, 4H), 3.14 (s, 4H), 2.26 (s, 3H)

(S)—N-(5-(4-methylphenylsulfonamido)-6-(4-morpholinophenylamino)-6-oxohexyl)-5-(trifluoromethyl)picolinamide

[0465] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.82 (s, 1H), 8.35 (d, J=8.00 Hz, 1H), 8.22 (s, 1H), 8.13 (d, J=8.00 Hz, 1H), 7.71 (d, J=8.00 Hz, 2H), 7.28-7.25 (m, 2H), 7.19 (d, J=8.40 Hz, 2H), 6.81 (d, J=8.80 Hz, 2H), 3.85 (t, J=4.80 Hz, 4H), 3.80-3.76 (m, 1H), 3.45-3.39 (m, 2H), 3.09 (t, J=4.60 Hz, 4H), 2.31 (s, 3H), 1.87-1.73 (m, 2H), 1.60-1.55 (m, 2H), 1.33-1.30 (m, 2H)

(S)-Benzyl 4-(4-methylphenylsulfonamido)-5-(4-morpholinophenylamino)-5-oxopentanoate

[0466] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.25 (s, 1H), 7.71 (d, J=8.00 Hz, 2H), 7.36-7.30 (m, 5H), 7.21 (d, J=8.80 Hz, 2H), 7.16 (d, J=8.00 Hz, 2H), 6.77 (d, J=8.80 Hz, 2H), 6.30 (d, J=7.60 Hz, 1H), 5.12-5.04 (m, 2H), 3.95-3.90 (m, 1H), 3.83 (t, J=4.60 Hz, 4H), 3.06 (t, J=4.80 Hz, 4H), 2.55-2.48 (m, 1H), 2.36-2.30 (m, 1H), 2.28 (s, 3H), 2.06-2.03 (m, 1H), 1.96-1.93 (m, 1H)

(S)-Benzyl 3-(4-methylphenylsulfonamido)-4-(4-morpholinophenylamino)-4-oxobutanoate

[0467] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.39 (s, 1H), 7.75 (d, J=8.00 Hz, 2H), 7.33-7.23 (m, 9H), 6.81 (d, J=8.80 Hz, 2H), 6.25 (d, J=8.80 Hz, 1H), 5.09-5.00 (m, 2H), 4.22-4.21 (m, 1H), 3.84 (t, J=4.80 Hz, 4H), 3.08 (t, J=4.80 Hz, 4H), 3.03 (dd, J=4.00, 17.2 Hz, 1H), 2.41 (dd, J=6.20, 17.4 Hz, 1H), 2.36 (s, 3H)

(S)-4-Methyl-N-(4-methyl-1-(4-morpholinophenylamino)-1-oxopentan-2-yl)benzamide

[0468] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.73 (s, 1H), 7.69 (d, J=8.00 Hz, 2H), 7.42 (d, J=8.00 Hz, 2H), 7.22 (d, J=8.80 Hz, 2H), 6.84-6.80 (m, 3H) 4.90-4.86 (m, 1H), 3.84 (t, J=4.80 Hz, 4H), 3.08 (t, J=4.80 Hz, 4H), 2.39 (s, 3H), 1.90-1.88 (m, 1H), 1.86-1.71 (m, 2H), 0.97 (d, J=6.40 Hz, 3H), 0.90 (d, J=6.40 Hz, 3H)

2-(4-Methylphenylsulfonamido)-N-(4-morpholinophenyl)acetamide

[0469] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.96 (s, 1H), 7.76 (d, J=8.40 Hz, 2H), 7.35-7.32 (m, 4H), 6.85 (d, J=8.80 Hz, 2H), 5.31 (t, J=6.80 Hz, 1H), 3.85 (t, J=4.80 Hz, 4H), 3.69 (d, J=6.40 Hz, 2H), 3.11 (t, J=4.80 Hz, 4H), 2.42 (s, 3H)

(S)-3-(4-Methylphenylsulfonamido)-4-(4-morpholinophenylamino)-4-oxobutanoic acid

[0470] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 9.77 (s, 1H), 7.65-7.20 (m, 4H), 7.21 (d, J=4.00 Hz, 2H), 6.82 (d, J=8.80 Hz, 2H), 4.17 (t, J=7.00 Hz, 1H), 3.72 (t, J=4.40 Hz, 4H), 3.02 (t, J=4.60 Hz, 4H), 2.57 (dd, J=16.2, 6.60 Hz, 1H), 2.35 (dd, J=16.0, 7.60 Hz, 1H), 2.25 (s, 3H)

(S)-4-(4-Methylphenylsulfonamido)-5-(4-morpholinophenylamino)-5-oxopentanoic acid

[0471] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 9.67 (s, 1H), 7.65 (d, J=8.40 Hz, 2H), 7.25 (d, J=7.60 Hz, 2H), 7.19 (d, J=8.80 Hz, 2H), 6.84 (d, J=8.40 Hz, 2H), 3.83-3.79 (m, 1H), 3.72 (t, J=4.60 Hz, 4H), 3.02 (t, J=4.80 Hz, 4H), 2.26 (s, 3H), 2.20-2.11 (m, 2H), 1.80-1.70 (m, 2H)

(S)-3-(4-hydroxyphenyl)-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)propanamide

[0472] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 9.61 (s, 1H), 9.18 (s, 1H), 8.05 (s, 1H), 7.49 (d, J=8.00 Hz, 2H), 7.15 (d, J=8.40 Hz, 4H), 6.93 (d, J=7.60 Hz, 2H), 6.82 (d, J=9.20 Hz, 2H), 6.57 (d, J=8.80 Hz, 2H), 3.98-3.85 (m, 1H), 3.72 (t, J=4.60 Hz, 4H), 3.01 (t, J=4.60 Hz, 4H), 2.78-2.73 (m, 1H), 2.67-2.59 (m, 1H), 2.33 (s, 3H)

(S)-3-(1H-Indol-3-yl)-2-(4-methylphenylsulfonamido)-N-phenylpropanamide

[0473] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.14 (s, 1H), 8.10 (s, 1H), 7.45 (d, J=8.40 Hz, 2H), 7.34 (d, J=7.60 Hz, 2H), 7.30-7.24 (m, 4H), 7.17-7.11 (m, 2H), 7.09-6.92 (m, 3H), 6.91 (s, 1H), 5.19 (d, J=5.60 Hz, 1H), 4.05-4.01 (m, 1H), 3.20-3.17 (m, 2H), 2.29 (s, 3H)

(S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-phenylpropanamide)

[0474] .sup.1H NMR (400 MHz, DMSO-d.sub.6) δ 10.78 (s, 1H), 9.98 (s, 1H), 8.40 (s, 1H), 7.40-7.39 (m, 5H), 7.36 (d, J=8.40 Hz, 2H), 7.30-7.23 (m, 3H), 7.10 (s, 1H), 7.06-7.01 (m, 2H), 6.93 (t, J=7.20 Hz, 1H), 4.16-4.13 (m, 1H), 3.05 (dd, J=14.2, 6.00 Hz, 1H), 2.87 (dd, J=14.7, 8.00 Hz, 1H)

(S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(thiophen-2-ylmethyl)propanamide

[0475] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.20 (s, 1H), 7.41 (d, J=8.40 Hz, 2H), 7.28-7.24 (m, 2H), 7.16-7.11 (m, 2H), 7.01-6.88 (m, 3H), 6.87 (s, 1H), 6.81 (s, 1H), 6.74 (s, 1H), 5.13 (d, J=6.00 Hz, 1H), 4.48-4.45 (m, 2H), 3.94-3.91 (m, 1H), 3.11-3.09 (m, 2H), 2.31 (s, 3H)

(S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(thiophen-2-ylmethyl)propanamide

[0476] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.73 (s, 1H), 8.62 (t, J=6.00 Hz, 1H), 8.22 (s, 1H), 7.42-7.33 (m, 6H), 7.27 (d, J=8.40 Hz, 1H), 7.05-7.01 (m, 2H), 6.94-6.88 (m, 2H), 6.86 (d, J=2.40 Hz, 1H), 4.30-4.26 (m, 2H), 3.99-3.95 (m, 1H), 2.99 (dd, J=14.2, 6.00 Hz, 1H), 2.80 (dd, J=14.7, 8.00 Hz, 1H)

(S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(2-methoxyphenyl)thiazol-2-yl)propanamide

[0477] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 12.39 (s, 1H), 10.76 (s, 1H), 8.48 (s, 1H), 7.64 (s, 1H), 7.47 (d, J=7.60 Hz, 1H), 7.41-7.11 (m, 6H), 7.08-7.01 (m, 5H), 6.91 (t, J=7.60 Hz, 1H), 4.34-4.30 (m, 1H), 3.91 (s, 3H), 3.12-3.07 (m, 1H), 2.91-2.85 (m, 1H)

(S)—N-(3-(N-(4-methyl-1-morpholino-1-oxopentan-2-yl)sulfamoyl)phenyl)acetamide

[0478] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.47 (s, 1H), 8.25 (d, J=8.80 Hz, 1H), 7.76 (t, J=1.80 Hz, 1H), 7.54 (d, J=7.60 Hz, 1H), 7.45 (t, J=8.00 Hz, 1H), 6.69 (d, J=9.60 Hz, 1H), 4.15-4.08 (m, 1H), 3.59-3.49 (m, 2H), 3.42-3.18 (m, 6H), 2.16 (s, 3H), 1.99-1.94 (m, 1H), 1.52-1.45 (m, 1H), 1.18-1.11 (m, 1H), 0.95 (d, J=6.80 Hz, 3H), 0.91 (d, J=6.80 Hz, 3H)

(S)-Benzyl 4-methyl-2-(3-phenylureido)pentanoate

[0479] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.38 (s, 1H), 7.34-7.01 (m, 8H), 6.99-6.97 (m, 1H), 5.83 (d, J=8.00 Hz, 1H), 5.19-5.07 (m, 2H), 4.65-4.60 (m, 1H), 1.71-1.57 (m, 2H), 1.51-1.46 (m, 1H), 0.91 (d, J=6.40 Hz, 3H), 0.88 (d, J=6.40 Hz, 3H)

4-Methyl-N-(2-morpholino-2-oxoethyl)benzenesulfonamide

[0480] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.76 (d, J=8.00 Hz, 2H), 7.30 (d, J=8.00 Hz, 2H), 6.20 (t, J=4.60 Hz, 1H), 3.79 (d, J=4.80 Hz, 2H), 3.58-3.62 (m, 4H), 3.51 (t, J=4.40 Hz, 2H), 3.32 (t, J=4.60 Hz, 2H), 2.4 (s, 3H) 4-Methyl-N-(1-(morpholine-4-carbonyl)cyclohexyl)benzenesulfonamide

[0481] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 7.79 (d, J=8.00 Hz, 2H), 7.29 (d, J=8.00 Hz, 2H), 5.33 (s, 1H), 3.74-3.78 (m, 8H), 2.43 (s, 3H), 1.74-1.91 (m, 4H), 1.17-1.40 (m, 6H).

(S)-4-(N-(4-methyl-1-oxo-1-(1,4,7-trioxa-10-azacyclododecan-10-yl)pentan-2-yl)sulfamoyl)benzoic acid

[0482] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.20 (d, J=8.40 Hz, 2H), 7.94 (d, J=8.40 Hz, 2H), 6.49 (d, J=9.20 Hz, 1H), 4.46-4.41 (m, 1H), 3.84-3.78 (m, 2H), 3.65-3.25 (m, 14H), 1.93-1.89 (m, 1H), 1.56-1.36 (m, 2H), 0.91 (t, J=7.00 Hz, 6H)

(S)-2-(4-Hydroxyphenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-morpholinophenyl)propanamide

[0483] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.78 (s, 1H), 10.18 (s, 1H), 9.64 (s, 1H), 7.84 (d, J=8.40 Hz, 1H), 7.50 (d, J=8.80 Hz, 2H), 7.39 (d, J=7.60 Hz, 1H), 7.29 (d, J=7.60 Hz, 1H), 7.22 (d, J=9.20 Hz, 2H), 7.06 (d, J=2.40 Hz, 1H), 7.03 (d, J=7.20 Hz, 1H), 6.93 (t, J=7.40 Hz, 1H), 6.82 (d, J=9.20 Hz, 2H), 6.70 (d, J=8.40 Hz, 2H), 4.08-4.02 (m, 1H), 3.72 (t, J=4.80 Hz, 4H), 3.07-3.00 (m, 5H), 2.84-2.79 (m, 1H)

(S)-4-(N-(3-(1-indol-3-yl)-1-(4-morpholinophenylamino)-1-oxopropan-2-yl)sulfamoyl)benzoic acid

[0484] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.77 (s, 1H), 9.83 (s, 1H), 8.43 (d, J=9.20 Hz, 1H), 7.76 (d, J=8.00 Hz, 2H), 7.63 (d, J=8.40 Hz, 2H), 7.44 (d, J=7.60 Hz, 1H), 7.26-7.22 (m, 3H), 7.09 (d, J=2.04 Hz, 1H), 7.00 (t, J=7.20 Hz, 1H), 6.91 (t, J=7.60 Hz, 3H), 4.14-4.12 (m, 1H), 3.76 (t, J=4.60 Hz, 4H), 3.07-3.03 (m, 5H), 2.90-2.86 (m, 1H)

(S)-2-Amino-3-(1-indol-3-yl)-N-(4-morpholinophenyl)propanamide

[0485] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 9.27 (s, 1H), 8.21 (s, 1H), 7.70 (d, J=8.00 Hz, 1H), 7.51-7.47 (m, 2H), 7.37 (d, J=8.40 Hz, 1H), 7.22-7.11 (m, 2H), 7.08 (d, J=2.40 Hz, 1H), 6.89-6.86 (m, 2H), 3.86-3.82 (m, 5H), 3.49-3.45 (m, 1H), 3.11 (t, J=4.80 Hz, 4H), 3.04-2.99 (m, 1H), 1.81 (s, 2H)

(S)—N-(4-(4-Acetylpiperazin-1-yl)-2-methoxyphenyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide

[0486] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.54 (s, 1H), 8.49 (s, 1H), 8.12 (d, J=8.40 Hz, 1H), 7.46 (d, J=8.40 Hz, 2H), 7.32-7.26 (m, 2H), 7.13 (t, J=7.60 Hz, 1H), 7.00-6.95 (m, 3H), 6.92 (d, J=2.40 Hz, 1H), 6.45-6.40 (m, 2H), 5.37 (d, J=5.60 Hz, 1H), 4.09-4.05 (m, 1H), 3.75 (t, J=5.40 Hz, 2H), 3.71 (s, 3H), 3.59 (t, J=5.00 Hz, 2H), 3.21-3.04 (m, 6H), 2.28 (s, 3H), 2.13 (s, 3H)

(S)—N-(4-(4-Acetylpiperazin-1-yl)phenyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide

[0487] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.31 (s, 1H), 8.11 (s, 1H), 8.47 (d, J=8.40 Hz, 2H), 7.31-7.25 (m, 5H), 7.16 (t, J=7.60 Hz, 1H), 7.04 (d, J=8.40 Hz, 2H), 6.99 (t, J=7.60 Hz, 1H), 6.94 (d, J=2.40 Hz, 1H), 6.82 (d, J=9.20 Hz, 2H), 5.22 (d, J=6.00 Hz, 1H), 4.02-4.00 (m, 1H), 3.74 (t, J=5.00 Hz, 2H), 3.59 (t, J=5.00 Hz, 2H), 3.18 (d, J=6.40 Hz, 2H), 3.10 (t, J=5.00 Hz, 2H), 3.05 (t, J=5.00 Hz, 2H), 2.31 (s, 3H), 2.12 (s, 3H)

(S)—N-(3-(1H-indol-3-yl)-1-(2-(4-morpholinobenzoyl)hydrazinyl)-1-oxopropan-2-yl)-4-methylbenzenesulfonamide

[0488] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.71 (s, 1H), 10.17 (s, 2H), 7.99 (s, 1H), 7.82 (d, J=8.80 Hz, 2H), 7.37 (d, J=8.00 Hz, 1H), 7.33 (d, J=8.40 Hz, 2H), 7.26 (d, J=7.26 Hz, 1H), 7.14 (s, 1H), 7.04-6.98 (m, 5H), 6.90 (t, J=7.40 Hz, 1H), 4.07 (s, 1H), 3.74 (t, J=4.40 Hz, 4H), 3.24 (t, J=4.80 Hz, 4H), 3.11-3.06 (m, 1H), 2.80-2.74 (m, 1H), 2.21 (s, 3H)

(S)-3-(1-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-(4-morpholinophenyl)thiazol-2-yl)propanamide

[0489] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 12.24 (s, 1H), 10.76 (s, 1H), 8.21 (s, 1H), 7.73 (d, J=8.80 Hz, 2H), 7.46 (d, J=8.00 Hz, 2H), 7.41 (d, J=8.00 Hz, 1H), 7.35 (s, 1H), 7.27 (d, J=8.40 Hz, 1H), 7.05-6.97 (m, 6H), 6.91 (t, J=7.60 Hz, 1H), 4.29 (s, 1H), 3.74 (t, J=4.60 Hz, 4H), 3.15 (t, J=4.60 Hz, 4H), 3.10-3.05 (m, 1H), 2.88-2.82 (m, 1H), 2.18 (s, 3H)

(S)-Methyl 4-(2-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)thiazol-4-yl)benzoate

[0490] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 12.39 (s, 1H), 10.77 (s, 1H), 8.25 (d, J=8.00 Hz, 1H), 8.02 (s, 4H), 7.81 (s, 1H), 7.46 (d, J=8.40 Hz, 2H), 7.42 (d, J=8.00 Hz, 1H), 7.27 (d, J=8.40 Hz, 1H), 7.06-7.01 (m, 4H), 6.91 (t, J=7.60 Hz, 1H), 4.32-4.30 (s, 1H), 3.86 (s, 3H), 3.12-3.06 (m, 1H), 2.90-2.84 (m, 1H), 2.17 (s, 3H)

(S)-Benzyl 3-(1H-indol-3-yl)-2-(6-(trifluoromethyl)pyridine-3-sulfonamido)propanoate

[0491] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.85 (d, J=1.60 Hz, 1H), 7.91 (s, 1H), 7.83 (dd, J=1.60, 8.40 Hz, 1H), 7.42 (d, J=8.40 Hz, 1H), 7.36-7.33 (m, 4H), 7.26-7.15 (m, 5H), 7.08-7.04 (m, 1H), 6.84 (d, J=2.40 Hz, 1H), 5.40 (d, J=8.80 Hz, 1H), 5.03 (s, 2H), 4.43-4.38 (m, 1H), 3.33-3.28 (m, 1H), 3.16-3.10 (m, 1H)

(S)-2-(4-Methylphenylsulfonamido)-N.SUP.1.-(morpholinophenyl)-N.SUP.5.-(4-nitrophenyl)pentanediamide

[0492] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.57 (s, 1H), 9.71 (s, 1H), 8.21 (d, J=8.80 Hz, 2H), 8.08 (s, 1H), 7.81 (d, J=9.20 Hz, 2H), 7.65 (d, J=8.40 Hz, 2H), 7.22-7.18 (m, 4H), 6.84 (d, J=8.80 Hz, 2H), 3.86 (t, J=6.80 Hz, 1H), 3.72 (t, J=4.60 Hz, 4H), 3.02 (t, J=4.80 Hz, 4H), 2.46-2.37 (m, 2H), 2.21 (s, 3H), 1.93-1.79 (m, 2H)

(S)-Benzyl 5-(4-methylphenylsulfonamido)-6-(4-morpholinophenylamino)-6-oxohexylcarbamate

[0493] .sup.1H-NMR (400 MHz, CD.sub.3OD) δ 7.71 (d, J=8.00 Hz, 2H), 7.32-7.25 (m, 5H), 7.22 (d, J=8.40 Hz, 2H), 7.15 (d, J=8.40 Hz, 2H), 6.86 (d, J=9.20 Hz, 2H), 5.06 (s, 2H), 3.82-3.78 (m, 5H), 3.07-3.03 (m, 6H), 2.26 (s, 3H), 1.69-1.59 (m, 2H), 1.48-1.28 (m, 4H)

(S)-6-Amino-2-(4-methylphenylsulfonamido)-N-(4-morpholinophenyl)hexanamide

[0494] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 9.65 (s, 1H), 7.65 (d, J=8.40 Hz, 2H), 7.25-7.19 (m, 4H), 6.83 (d, J=8.80 Hz, 2H), 3.77-3.71 (m, 5H), 3.02 (t, J=4.80 Hz, 4H), 2.42 (t, J=6.40 Hz, 2H), 2.26 (s, 3H), 1.52-1.44 (m, 2H), 1.24-1.12 (m, 4H)

(S)-3,5-Dimethoxy-N-(5-(4-methylphenylsulfonamido)-6-(4-morpholinophenylamino)-6-oxohexyl)benzamide

[0495] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.60 (s, 1H), 7.68 (d, J=8.00 Hz, 2H), 7.25 (d, J=8.80 Hz, 2H), 7.14 (d, J=8.40 Hz, 2H), 6.98 (d, J=2.40 Hz, 2H), 6.77 (d, J=9.20 Hz, 2H), 6.86 (t, J=6.00 Hz, 1H), 6.58 (s, 1H), 6.35 (d, J=7.20 Hz, 1H), 3.83 (t, J=4.60 Hz, 4H), 3.78-3.75 (m, 7H), 3.39-3.32 (m, 2H), 3.06 (t, J=4.80 Hz, 4H), 2.26 (s, 3H), 1.85-1.71 (m, 2H), 1.52-1.47 (m, 2H), 1.30-1.23 (m, 2H)

(S)—N.SUP.5.-(4-Methoxybenzyl)-2-(4-methylphenylsulfonamido)-N.SUP.1.-(4-morpholinophenyl)pentanediamide

[0496] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 9.60 (s, 1H), 8.25 (t, J=5.80 Hz, 1H), 7.95 (s, 1H), 7.64 (d, J=8.40 Hz, 2H), 7.23 (d, J=8.40 Hz, 2H), 7.19 (d, J=9.20 Hz, 2H), 7.14 (d, J=8.80 Hz, 2H), 6.84 (t, J=8.80 Hz, 4H), 4.15 (d, J=6.00 Hz, 2H), 3.82-3.71 (m, 8H), 3.02 (t, J=4.80 Hz, 4H), 2.26 (s, 3H), 2.17-2.05 (m, 2H), 1.82-1.75 (m, 2H)

(S)-2-(4-Methylphenylsulfonamido)-N.SUP.1.-(4-morpholinophenyl)-N.SUP.5.-phenylpentanediamide

[0497] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 9.89 (s, 1H), 9.64 (s, 1H), 7.98 (s, 1H), 7.66 (d, J=8.00 Hz, 2H), 7.56 (d, J=8.40 Hz, 2H), 7.28-7.19 (m, 6H), 7.01 (t, J=7.40 Hz, 1H), 6.84 (d, J=8.80 Hz, 2H), 3.86 (t, J=6.80 Hz, 1H), 3.72 (t, J=4.60 Hz, 4H), 3.02 (t, J=4.60 Hz, 4H), 2.41-2.26 (m, 2H), 2.23 (s, 3H), 1.94-1.80 (m, 2H)

(S)-2-(4-Methylphenylsulfonamido)-5-morpholino-N-(4-morpholinophenyl)-5-oxopentanamide

[0498] .sup.1H-NMR (400 MHz, CDCl.sub.3) δ 8.75 (s, 1H), 7.74 (d, J=8.40 Hz, 2H), 7.34 (d, J=8.80 Hz, 2H), 7.28 (d, J=8.00 Hz, 2H), 7.11 (d, J=6.00 Hz, 1H), 8.65 (d, J=8.80 Hz, 2H), 3.86 (t, J=4.60 Hz, 1H), 3.78-3.65 (m, 6H), 3.59-3.55 (m, 1H), 3.45-3.33 (m, 2H), 3.10 (t, J=5.00 Hz, 4H), 2.64-2.63 (m, 2H), 2.38 (s, 3H), 2.23-2.18 (m, 2H), 2.07-2.02 (m, 2H)

(S)—N.SUP.5.-(4-fluorophenyl)-2-(4-methylphenylsulfonamido)-N.SUP.1.-(4-morpholinophenyl)pentanediamide

[0499] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 9.99 (s, 1H), 9.68 (s, 1H), 8.04 (s, 1H), 7.65 (d, J=8.00 Hz, 2H), 7.58-7.55 (m, 2H), 7.21 (t, J=8.00 Hz, 4H), 7.12 (t, J=8.80 Hz, 2H), 6.84 (d, J=8.80 Hz, 2H), 3.85 (s, 1H), 3.72 (s, 4H), 3.02 (s, 4H), 2.38-2.26 (m, 2H), 2.22 (s, 3H), 1.89-1.81 (m, 2H)

(S)—N.SUP.5.-(4-tert-butylphenyl)-2-(4-methylphenylsulfonamido)-N.SUP.1.-(4-morpholinophenyl)pentanediamide

[0500] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 9.86 (s, 1H), 9.69 (s, 1H), 8.05 (s, 1H), 7.65 (d, J=8.40 Hz, 2H), 7.47 (d, J=8.80 Hz, 2H), 7.29 (d, J=8.80 Hz, 2H), 7.22-7.19 (m, 4H), 6.84 (d, J=8.80 Hz, 2H), 3.84 (t, J=6.80 Hz, 1H), 3.73 (t, J=4.60 Hz, 4H), 3.02 (t, J=4.80 Hz, 4H), 2.40-2.25 (m, 2H), 2.22 (s, 3H), 1.92-1.77 (m, 2H), 1.24 (s, 9H)

(S)-2-(4-Methylphenylsulfonamido)-M-(4-morpholinophenyl)-N.SUP.5.-(4-(trifluoromethyl)phenyl)pentanediamide

[0501] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.30 (s, 1H), 9.69 (s, 1H), 8.05 (s, 1H), 7.77 (d, J=8.80 Hz, 2H), 7.65 (d, J=8.00 Hz, 4H), 7.22-7.19 (m, 4H), 6.84 (d, J=8.80 Hz, 2H), 3.86 (s, 1H), 3.72 (s, 4H), 3.02 (s, 4H), 2.44-2.33 (m, 2H), 2.21 (s, 3H), 1.93-1.82 (m, 2H)

(S)-2-(4-Methylphenylsulfonamido)-N.SUP.1.-(4-morpholinophenyl)-N.SUP.4.-(4-nitrophenyl)succinamide

[0502] .sup.1H-NMR (400 MHz, DMSO-d.sub.6) δ 10.55 (s, 1H), 9.80 (s, 1H), 8.21 (d, J=8.80 Hz, 2H), 8.18 (s, 1H), 7.75 (d, J=9.20 Hz, 2H), 7.65 (d, J=8.40 Hz, 2H), 7.25 (d, J=8.80 Hz, 2H), 7.18 (d, J=8.40 Hz, 2H), 6.84 (d, J=8.80 Hz, 2H), 4.35 (t, J=6.80 Hz, 1H), 3.72 (t, J=4.60 Hz, 4H), 3.02 (t, J=4.80 Hz, 4H), 2.78 (dd, J=6.60, 15.40 Hz, 1H), 2.62 (dd, J=7.80, 15.40 Hz, 1H), 2.21 (s, 3H)

(S)—N-(furan-2-ylmethyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide

[0503] .sup.1H-NMR (500 MHz, CDCl.sub.3) δ 8.10 (s, 1H), 7.45-7.43 (d, J=10.00 Hz, 2H), 7.32 (s, 1H), 7.31-7.30 (d, J=5.00 Hz, 1H), 7.26-7.25 (d, J=5.00 Hz, 1H), 7.18-7.15 (t, J=7.50 Hz, 1H), 7.06-7.05 (d, J=5.00 Hz, 2H), 7.01-6.98 (t, J=7.50 Hz, 1H), 6.83 (s, 1H), 6.67 (s, 1H), 6.30 (s, 1H), 6.15 (s, 1H), 4.97-4.96 (d, J=0.94 Hz, 1H), 4.40-4.31 (m, 2H), 3.93-3.90 (m, 1H), 3.15-3.07 (m, 2H), 2.34 (s, 3H)

(S)-2-(4-Bromophenylsulfonamido)-N-(furan-2-ylmethyl)-3-(1H-indol-3-yl)propanamide

[0504] .sup.1H-NMR (500 MHz, CDCl.sub.3) δ 8.64 (s, 1H), 7.98 (s, 3H), 7.32-7.22 (m, 6H), 7.18-7.15 (t, J=7.50 Hz, 1H), 6.88 (s, 1H), 6.29 (s, 1H), 6.15 (s, 1H), 5.69 (s, 1H), 4.33 (m, 2H), 3.95-3.91 (m, 1H), 3.28-3.24 (m, 1H), 3.05-3.00 (m, 1H)

(S)-3-(1H-indol-3-yl)-N-isopropyl-2-(4-methylphenylsulfonamido)propanamide

[0505] .sup.1H-NMR (500 MHz, CDCl.sub.3) δ 8.27 (s, 1H), 7.47-7.45 (d, J=10.00 Hz, 2H), 7.33-7.31 (d, J=10.00 Hz, 2H), 7.19-7.16 (t, J=7.50 Hz, 1H), 7.07-7.05 (d, J=10.00 Hz, 2H), 7.02-6.99 (t, J=7.50 Hz, 1H), 6.92 (s, 1H), 6.02-6.00 (d, J=10.00 Hz, 1H), 5.09-5.07 (d, J=10.00 Hz, 1H), 3.97-3.90 (m, 1H), 3.86-3.82 (m, 1H), 3.15-3.07 (m, 2H), 2.33 (s, 3H)

(S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-isopropylpropanamide

[0506] .sup.1H-NMR (500 MHz, MeOD) δ 10.23 (s, 1H), 7.97-7.95 (d, J=5.00 Hz, 1H), 7.50-7.48 (d, J=10.00 Hz, 2H), 7.42-7.41 (d, J=5.00 Hz, 1H), 7.27-7.25 (d, J=10.00 Hz, 1H), 7.06-7.02 (m, 4H), 6.94-6.90 (m, 2H), 6.86-6.84 (d, J=10.00 Hz, 1H), 6.80-6.76 (t, J=10.00 Hz, 1H), 4.66 (s, 1H), 4.15-4.12 (t, J=7.50 Hz, 1H), 3.22-3.18 (m, 1H), 3.03-2.99 (m, 1H), 2.11 (s, 3H)

(S)—N-(3-(1H-indol-3-yl)-1-(2-(4-methoxybenzoyl)hydrazinyl)-1-oxopropan-2-yl)-4-methylbenzenesulfonamide

[0507] .sup.1H-NMR (500 MHz, CDCl.sub.3) δ 7.86-7.64 (d, J=8.50 Hz, 2H), 7.31-7.26 (m, 4H), 7.11-7.08 (t, J=7.50 Hz, 1H), 7.04 (s, 1H), 6.95-6.91 (m, 3H), 6.89-6.87 (d, J=8.00 Hz, 2H), 4.10-4.07 (m, 1H), 3.85 (s, 3H), 3.35-3.31 (m, 1H), 3.04-3.00 (m, 1H), 2.26 (s, 3H)

(S)-2-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanoyl)-N-(4-methoxyphenyl)hydrazinecarboxamide

[0508] .sup.1H-NMR (500 MHz, MeOD) δ 7.39-7.36 (t, J=7.00 Hz, 4H), 7.28-7.26 (d, J=8.00 Hz, 1H), 7.22-7.20 (d, J=7.50 Hz, 1H), 7.08-7.05 (t, J=7.50 Hz, 1H), 7.01 (s, 1H), 6.98 (s, 1H), 6.97 (s, 1H), 6.89-6.84 (m, 3H), 3.89-3.86 (m, 1H), 3.76 (s, 3H), 3.25-3.21 (m, 1H), 2.93-2.89 (m, 1H), 2.30 (s, 3H)

(S)-4-Bromo-N-(1-(3,5-dimethyl-1H-pyrazol-1-yl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)benzenesulfonamide

[0509] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 10.76 (s, 1H), 8.65 (s, 1H), 7.66-7.65 (d, J=9.50 Hz, 1H), 7.30-7.27 (t, J=7.50 Hz, 3H), 7.16-7.15 (d, J=8.00 Hz, 2H), 7.10 (s, 1H), 7.07-7.04 (t, J=7.50 Hz, 1H), 6.96-6.93 (t, J=7.50 Hz, 1H), 6.24 (s, 2H), 5.39-5.37 (d, J=8.50 Hz, 1H), 3.20-3.16 (d, J=14.00, 3.00 Hz, 1H), 2.89-2.84 (d, J=14.00, 10.50 Hz, 1H), 2.92 (s, 3H), 2.27 (s, 3H)

(S)—N-(3-(1H-indol-3-yl)-1-oxo-1-(3-phenyl-1H-pyrazol-1-yl)propan-2-yl)-4-bromobenzenesulfonamide

[0510] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 10.77 (s, 1H), 8.86 (s, 1H), 8.48 (s, 1H), 8.00-7.98 (d, J=7.50 Hz, 2H), 7.69-7.68 (d, J=7.50 Hz, 1H), 7.58-7.55 (t, J=7.00 Hz, 2H), 7.52-7.49 (t, J=7.50 Hz, 1H), 7.29-7.23 (m, 4H), 7.17 (s, 1H), 7.15 (s, 1H), 7.11-7.04 (m, 2H), 6.98-6.92 (m, 1H), 5.50-5.49 (d, J=7.00 Hz, 1H), 3.28-3.25 (d, J=14.00, 4.00 Hz, 1H), 2.97-2.92 (d, J=14.00, 10.00 Hz, 1H)

N—((S)-1-(2-((3S,5S,7S)-adamantane-1-carbonyl)hydrazinyl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-4-methylbenzenesulfonamide

[0511] .sup.1H-NMR (500 MHz, MeOD) δ 7.33-7.32 (d, J=8.00 Hz, 1H), 7.25-7.20 (t, J=7.50 Hz, 3H), 7.06-7.03 (t, J=7.50 Hz, 1H), 7.00 (s, 1H), 6.91-6.88 (t, J=8.00 Hz, 1H), 6.85-6.83 (d, J=8.00 Hz, 2H), 4.04-4.01 (d, J=9.50, 4.50 Hz, 1H), 3.29-3.25 (d, J=15.00, 5.00 Hz, 1H), 2.94-2.89 (d, J=15.00, 10.00 Hz, 1H), 2.24 (s, 3H), 2.02-2.01 (d, J=6.00 Hz, 3H), 1.95 (s, 6H), 1.80-1.74 (t, J=12.50 Hz, 6H)

(S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(p-tolyl)thiazol-2-yl)propanamide

[0512] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 12.47 (s, 1H), 10.79 (s, 1H), 8.53-8.52 (d, J=7.50 Hz, 1H), 7.78-7.77 (d, J=8.00 Hz, 2H), 7.55 (s, 1H), 7.48-7.47 (d, J=7.50 Hz, 1H), 7.44-7.37 (m, 4H), 7.29-7.27 (d, J=8.00 Hz, 1H), 7.25-7.23 (d, J=8.50 Hz, 2H), 7.09 (d, J=2.50 Hz, 1H), 7.06-7.03 (t, J=7.50 Hz, 1H), 6.94-6.91 (t, J=7.50 Hz, 1H), 4.35-4.31 (m, 1H), 3.12-3.08 (d, J=14.50, 6.50 Hz, 1H), 2.91-2.86 (d, J=15.00, 10.00 Hz, 1H), 2.33 (s, 3H)

(S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-phenethylpropanamide

[0513] .sup.1H-NMR (500 MHz, CDCl.sub.3) δ 8.27 (s, 1H), 8.02 (s, 1H), 7.47-7.46 (d, J=10.00 Hz, 2H), 7.32-7.31 (d, J=5.00 Hz, 2H), 7.28-7.25 (d, J=7.50 Hz, 2H), 7.23-7.22 (d, J=5.00 Hz, 1H), 7.20-7.17 (t, J=7.50 Hz, 1H), 7.08-7.01 (m, 5H), 6.84 (s, 1H), 6.37-6.35 (t, J=5.00 Hz, 1H), 5.08-5.07 (d, J=5.00 Hz, 1H), 3.43-3.35 (m, 2H), 3.10-3.07 (t, J=7.50 Hz, 2H), 2.70-2.59 (m, 2H), 2.35 (s, 3H)

(S)-2-(4-Bromophenylsulfonamido)-N-(4-(4-fluorophenyl)thiazol-2-yl)-3-(1H-Indol-3-yl)propanamide

[0514] .sup.1H-NMR (500 MHz, MeOD) δ 7.91-7.88 (m, 2H), 7.45-7.42 (m, 3H), 7.32 (s, 1H), 7.30-7.27 (m, 3H), 7.14-7.10 (t, J=10.00 Hz, 2H), 7.09-7.06 (t, J=7.50 Hz, 1H), 7.02 (s, 1H), 6.97-6.94 (t, J=7.50 Hz, 1H), 4.31-4.28 (m, 1H), 3.28-3.24 (m, 1H), 3.08-3.03 (m, 1H)

(S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(4-nitrophenyl)thiazol-2-yl)propanamide

[0515] .sup.1H-NMR (500 MHz, MeOD) δ 8.28-8.26 (d, J=10.00 Hz, 2H), 8.12-8.10 (d, J=10.00 Hz, 2H), 7.68 (s, 1H), 7.47-7.44 (m, 3H), 7.31-7.27 (m, 3H), 7.09-7.06 (t, J=7.50 Hz, 1H), 6.97-6.94 (t, J=7.50 Hz, 1H), 4.31-4.28 (m, 1H), 3.29-3.25 (m, 1H), 3.10-3.05 (m, 1H)

(S)—N-(3-(1H-Indol-3-yl)-1-(2-(4-methoxybenzoyl)hydrazinyl)-1-oxopropan-2-yl)-4-methylbenzenesulfonamide

[0516] .sup.1H-NMR (500 MHz, MeOD) δ 7.89-7.88 (d, J=8.50 Hz, 2H), 7.43-7.41 (d, J=8.80 Hz, 1H), 7.28-7.26 (d, J=8.00 Hz, 1H), 7.22-7.21 (d, J=8.50 Hz, 2H), 7.16-7.14 (d, J=8.00 Hz, 2H), 7.10-7.07 (t, J=7.00 Hz, 1H), 7.03-7.01 (d, J=11.00 Hz, 3H), 6.96-6.93 (t, J=7.00 Hz, 1H), 4.18-4.15 (d, J=10.00, 5.00 Hz, 1H), 3.87 (s, 3H), 3.35-3.32 (m, 1H), 3.00-2.95 (d, J=10.50, 4.00 Hz, 1H)

(S)-2-(4-Bromophenylsulfonamido)-N-(4-(4-cyanophenyl)thiazol-2-yl)-3-(1H-Indol-3-yl)propanamide

[0517] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 2.88-2.93 (dd, J=14.18, 8.80 Hz, 1H), 3.09-3.13 (dd, J=14.18, 6.35 Hz, 1H), 4.34-4.35 (d, J=6.35 Hz, 1H), 6.91-6.94 (t, J=7.33 Hz, 1H), 7.02-7.05 (t, J=7.82 Hz, 1H), 7.09-7.10 (d, J=1.95 Hz, 1H), 7.27-7.28 (d, J=8.31 Hz, 1H), 7.37-7.42 (m, 4H), 7.47-7.48 (d, J=7.82 Hz, 1H), 7.88-7.91 (m, 3H), 8.05-8.06 (d, J=8.31 Hz, 2H), 8.55-8.57 (d, J=7.33 Hz, 1H), 10.80 (s, 1H), 12.55 (brs, 1H)

(S)-2-(4-Bromophenylsulfonamido)-3-(1H-Indol-3-yl)-N-(4-(4-(trifluoromethyl)phenyl)thiazol-2-yl)propanamide

[0518] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 2.88-2.92 (dd, J=14.18, 8.80 Hz, 1H), 3.09-3.13 (dd, J=14.18, 6.35 Hz, 1H), 4.33-4.35 (m, 1H), 6.90-6.93 (t, J=7.33 Hz, 1H), 7.02-7.05 (t, J=7.33 Hz, 1H), 7.09 (d, J=1.95 Hz, 1H), 7.27-7.28 (d, J=8.31 Hz, 1H), 7.37-7.42 (q, J=8.31, 8.80, 7.82 Hz, 4H), 7.47-7.48 (d, J=7.82 Hz, 1H), 7.78-7.80 (d, J=8.31 Hz, 2H), 7.85 (s, 1H), 8.08-8.10 (d, J=8.31 Hz, 2H), 8.52-8.54 (d, J=7.33 Hz, 1H), 10.78 (s, 1H), 12.54 (brs, 1H).

(S)-4-Bromo-N-(1-(2-dodecanoylhydrazinyl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)benzenesulfonamide

[0519] .sup.1H-NMR (500 MHz, CDCl.sub.3) δ 0.86-0.89 (t, J=6.84 Hz, 3H), 1.26 (s, 16H), 1.51-1.54 (t, J=6.35 Hz, 2H), 2.30-2.37 (m, 2H), 3.13-3.17 (dd, J=14.67, 7.82 Hz, 1H), 3.22-3.26 (dd, J=14.67, 5.86 Hz, 1H), 4.36-4.38 (t, J=6.84 Hz, 1H), 7.02 (s, 1H), 7.06-7.09 (t, J=7.33 Hz, 1H), 7.18-7.21 (t, J=7.33 Hz, 1H), 7.32-7.34 (d, J=8.31 Hz, 1H), 7.38-7.39 (d, J=8.31 Hz, 2H), 7.42-7.44 (d, J=7.82 Hz, 1H), 7.47-7.48 (d, J=8.31 Hz, 2H), 8.34 (brs, 1H)

(S)-4-Bromo-N-(1-(2-decanoylhydrazinyl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)benzenesulfonamide

[0520] .sup.1H-NMR (500 MHz, CDCl.sub.3) δ 0.87-0.89 (t, J=6.35 Hz, 3H), 1.28 (s, 12H), 1.50-1.54 (m, 2H), 2.28-2.39 (m, 2H), 3.13-3.23 (dd, J=14.67, 7.33 Hz, 1H), 3.23-3.27 (dd, J=14.67, 5.38 Hz, 1H), 4.36-4.39 (t, J=6.84 Hz, 1H), 7.02 (s, 1H), 7.06-7.09 (t, J=7.82 Hz, 1H), 7.19-7.22 (t, J=7.33 Hz, 1H), 7.33-7.34 (d, J=8.31 Hz, 1H), 7.39-7.40 (d, J=8.31 Hz, 2H), 7.42-7.44 (d, J=7.82 Hz, 1H), 7.47-7.48 (d, J=8.31 Hz, 2H), 8.33 (brs. 1H)

(S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-phenethylpropanamide

[0521] .sup.1H-NMR (500 MHz, CDCl.sub.3) δ 2.60-2.73 (m, 2H), 2.93-2.98 (dd, J=14.18, 7.82 Hz, 1H), 3.17-3.21 (dd, J=14.67, 5.38 Hz, 1H), 3.33-3.40 (dq, J=13.69, 6.84×3 Hz, 1H), 3.43-3.49 (dq, J=13.20, 6.84×2, 6.35 Hz, 1H), 3.83-3.87 (q, J=6.35×2, 6.84 Hz, 1H), 5.26-5.27 (d, J=6.35 Hz, 1H), 6.36-6.38 (t, J=5.38 Hz, 1H), 6.82 (s, 1H), 7.00-7.03 (t, J=7.33 Hz, 1H), 7.06-7.08 (d, J=7.82 Hz, 2H), 7.19-7.31 (m, 10H), 8.16 (brs, 1H)

N—((S)-1-(2-((3S,5S,7S)-adamantane-1-carbonyl)hydrazinyl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-4-bromobenzenesulfonamide

[0522] .sup.1H-NMR (500 MHz, CDCl.sub.3) δ 1.66-1.75 (m, 6H), 1.89 (s, 6H), 2.03 (s, 3H), 3.03-3.07 (dd, J=14.67, 9.29 Hz, 1H), 3.26-3.30 (dd, J=15.16, 4.89 Hz, 1H), 4.27 (brs, 1H), 6.54 (brs, 1H), 6.96-7.01 (m, 2H), 7.13-7.18 (m, 3H), 7.24-7.32 (m, 4H), 8.32 (brs, 1H), 8.49 (brs, 1H), 9.66 (brs, 1H)

(S)-2-(4-Bromophenylsulfonamido)-N-(4-fluorophenethyl)-3-(1H-indol-3-yl)propanamide

[0523] .sup.1H-NMR (500 MHz, CDCl.sub.3) δ 2.59-2.71 (m, 2H), 2.92-3.00 (m, 1H), 3.18-3.22 (dd, J=14.67, 5.86 Hz, 1H), 3.31-3.37 (m, 1H), 3.43-3.49 (m, 1H), 3.83-3.87 (m, 1H), 5.19-5.22 (m, 1H), 6.41-6.43 (m, 1H), 6.86-7.04 (m, 5H), 7.20-7.35 (m, 7H), 8.17-7.20 (m, 1H)

(S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-methoxyphenethyl)propanamide

[0524] .sup.1H-NMR (500 MHz, CDCl.sub.3) δ 2.55-2.67 (m, 2H), 2.95-3.00 (m, 1H), 3.17-3.21 (m, 1H), 3.32-3.35 (m, 1H), 3.41-3.45 (m, 1H), 3.77-3.78 (d, J=4.40 Hz, 3H), 3.86 (m, 1H), 5.21-5.23 (t, J=4.40 Hz, 1H), 6.34-6.35 (d, J=4.40 Hz, 1H), 6.80-6.82 (m, 3H), 6.98-7.05 (m, 3H), 7.20-7.33 (m, 7H), 8.17 (brs, 1H)

(S)-2-(4-Bromophenylsulfonamido)-3-(1H-indol-3-yl)-N-(3-phenylpropyl)propanamide

[0525] .sup.1H-NMR (500 MHz, CDCl.sub.3) δ 1.69-1.74 (m, 2H), 2.53-2.56 (t, 6.84 Hz, 2H), 2.95-2.99 (dd, J=14.67, 6.84 Hz, 1H), 3.13-3.19 (m, 1H), 3.22-3.26 (dd, J=13.20, 5.86 Hz, 2H), 3.83-3.86 (m, 1H), 5.20-5.21 (d, J=3.91 Hz, 1H), 6.37 (brs, 1H), 6.90 (s, 1H), 7.00-7.03 (m, 1H), 7.11-7.12 (d, J=7.33 Hz, 2H), 7.17-7.31 (m, 10H), 8.15 (brs, 1H)

(S)—N((3R,5R,7R)-adamantan-1-yl)-2-(4-bromophenylsulfonamido)-3-(1H-Indol-3-yl)propanamide

[0526] .sup.1H-NMR (500 MHz, CDCl.sub.3) δ 1.58-1.64 (m, 6H), 1.74-1.80 (m, 6H), 2.01 (s, 3H), 3.05-3.09 (dd, J=14.67, 7.33 Hz, 1H), 3.15-3.20 (dd, J=14.67, 6.84 Hz, 1H), 3.77-3.81 (q, J=7.33, 6.84, 6.35 Hz, 1H), 5.35-5.36 (d, J=6.35 Hz, 1H), 5.65 (s, 1H), 6.96 (d, J=1.95 Hz, 1H), 7.04-7.07 (t, J=7.82 Hz, 1H), 7.20-7.23 (t, J=7.82 Hz, 1H), 7.33-7.39 (m, 6H), 8.21 (brs, 1H)

(S)—N-(3-(1H-indol-3-yl)-1-(4-(4-methoxyphenyl)piperazin-1-yl)-1-oxopropan-2-yl)-4-bromobenzenesulfonamide

[0527] .sup.1H-NMR (500 MHz, CDCl.sub.3) δ 1.77-1.80 (t, J=8.31 Hz, 1H), 2.34-2.41 (m, 2H), 2.62-2.66 (m, 1H), 2.78-2.81 (m, 1H), 2.92-2.97 (m, 1H), 3.10-3.16 (m, 2H), 3.19-3.23 (m, 1H), 3.38-3.42 (m, 1H), 3.76 (s, 3H), 4.48-4.53 (m, 1H), 6.02-6.04 (d, J=9.78 Hz, 1H), 6.68-6.66 (m, 2H), 6.77-6.80 (m, 2H), 7.04 (d, J=2.44 Hz, 1H), 7.11-7.14 (t, J=7.82 Hz, 1H), 7.17-7.20 (t, J=7.33 Hz, 1H), 7.30-7.31 (d, J=8.31 Hz, 1H), 7.50-7.54 (m, 3H), 7.62-7.64 (d, J=8.31 Hz, 2H), 8.11 (brs, 1H)

(S)—N-(3-(1H-indol-3-yl)-1-(4-(4-methoxyphenyl)piperazin-1-yl)-1-oxopropan-2-yl)-4-methylbenzenesulfonamide

[0528] .sup.1H-NMR (500 MHz, CDCl.sub.3) δ 1.65-1.69 (m, 1H), 2.21-2.24 (m, 1H), 2.28-2.37 (m, 4H), 2.53-2.56 (m, 1H), 2.66-2.69 (m, 1H), 2.81-2.84 (m, 1H), 3.04-3.15 (m, 2H), 3.21-3.25 (dd, J=13.69, 4.89 Hz, 1H), 3.32-3.35 (m, 1H), 3.75 (s, 3H), 4.45-4.50 (td, J=5.38×2, 4.40 Hz, 1H), 5.91-5.93 (d, J=9.78 Hz, 1H), 6.59-6.61 (d, J=9.29 Hz, 2H), 6.77-6.79 (d, J=9.29 Hz, 2H), 7.05-7.06 (d, J=2.44 Hz, 1H), 7.10-7.13 (t, J=7.82 Hz, 1H), 7.16-7.19 (t, J=7.33 Hz, 1H), 7.20-7.22 (d, J=8.31 Hz, 2H), 7.29-7.31 (d, J=7.82 Hz, 1H), 7.51-7.53 (d, J=7.82 Hz, 1H), 7.68-7.70 (d, J=8.31 Hz, 2H, 8.14 (brs, 1H)

(S)—N-((3R,5R,7R)-adamantan-1-yl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide

[0529] .sup.1H-NMR (500 MHz, CDCl.sub.3) δ 1.57-1.64 (m, 6H), 1.74-1.80 (m, 6H), 2.00 (brs, 3H), 2.34 (s, 3H), 3.04-3.08 (m, 1H), 3.12-3.16 (m, 1H), 3.78-3.82 (q, J=6.84, 6.35×2 Hz, 1H), 5.13-5.14 (d, J=6.35 Hz, 1H), 5.75 (s, 1H), 6.94-6.95 (d, J=1.46 Hz, 1H), 7.01-7.04 (t, J=7.33 Hz, 1H), 7.08-7.09 (d, J=7.82 Hz, 2H), 7.15-7.19 (m, 1H), 7.32-7.36 (t, J=8.80 Hz, 2H), 7.48-7.50 (d, J=8.31 Hz, 2H), 8.27 (brs, 1H)

(S)-3-(1H-indol-3-yl)-N-(4-methoxyphenethyl)-2-(4-methylphenylsulfonamido)propanamide

[0530] .sup.1H-NMR (500 MHz, CDCl.sub.3) δ 2.33 (s, 3H), 2.50-2.63 (m, 2H), 3.01-3.10 (m, 2H), 3.30-3.40 (m, 2H), 3.77 (s, 3H), 3.85-3.89 (q, J=6.35 Hz, 1H), 5.03-5.04 (d, J=5.86 Hz, 1H), 6.36-6.38 (t, 5.38 Hz, 1H), 6.77-6.81 (m, 3H), 6.93-6.95 (d, J=8.80 Hz, 2H), 6.98-7.01 (t, J=7.33 Hz, 1H), 7.04-7.06 (d, J=7.82 Hz, 2H), 7.15-7.18 (t, J=7.82 Hz, 1H), 7.26-7.31 (m, 2H), 7.43-7.45 (d, J=8.31 Hz, 2H), 8.22 (brs, 1H)

(S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(3-phenylpropyl)propanamide

[0531] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 1.40-1.46 (m, 2H), 2.23 (s, 3H), 2.34-2.37 (t, J=7.33 Hz, 2H), 2.75-2.83 (m, 3H), 2.94-2.99 (dd, J=14.18, 6.84 Hz, 1H), 3.89-3.92 (t, J=6.84 Hz, 1H), 6.90-6.93 (t, J=7.33 Hz, 1H), 7.01-7.04 (t, J=7.33 Hz, 1H), 7.07-7.17 (m, 6H), 7.24-7.28 (m, 3H), 7.34-7.36 (d, J=7.82 Hz, 1H), 7.48-7.49 (d, J=7.82 Hz, 2H), 7.85-7.87 (t, J=5.38 Hz, 1H), 7.93 (brs, 1H), 10.77 (s, 1H)

(S)—N-(4-fluorophenethyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide

[0532] .sup.1H-NMR (500 MHz, CD.sub.3OD) δ 2.28 (s, 3H), 2.49-2.54 (m, 2H), 2.80-2.84 (dd, J=14.18, 7.82 Hz, 1H), 3.07-3.14 (m, 2H), 3.23-3.27 (m, 1H), 3.86-3.89 (t, J=7.82 Hz, 1H), 6.92-7.06 (m, 9H), 7.26-7.27 (d, J=7.82 Hz, 1H), 7.31-7.33 (d, J=7.82 Hz, 1H), 7.40-7.42 (d, J=7.82 Hz, 2H)

(S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)-N-(4-(4-(trifluoromethyl)phenyl)thiazol-2-yl)propanamide

[0533] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 2.15 (s, 3H), 2.85-2.90 (dd, J=14.67, 7.82 Hz, 1H), 3.07-3.11 (dd, J=14.67, 6.84 Hz, 1H), 4.28-4.31 (t, J=7.33 Hz, 1H), 6.89-6.92 (t, J=7.33 Hz, 1H), 7.01-7.06 (m, 4H), 7.26-7.28 (d, J=8.31 Hz, 1H), 7.40-7.42 (d, J=7.82 Hz, 1H), 7.45-7.47 (d, J=8.31 Hz, 2H), 7.78-7.80 (m, 3H), 8.06-8.08 (d, J=8.31 Hz, 2H), 8.27 (brs, 1H), 10.78 (s, 1H), 12.39 (brs, 1H)

(S)—N-(2-(1H-indol-3-yl)ethyl)-2-(4-bromophenylsulfonamido)-3-(1H-indol-3-yl)propanamide

[0534] .sup.1H-NMR (500 MHz, CD.sub.3OD) δ 2.72-2.84 (m, 3H), 3.14-3.18 (dd, J=14.67, 5.38 Hz, 1H), 3.27-3.30 (m, 1H), 3.38-3.42 (m, 1H), 3.92-3.95 (dd, 9.29, 5.38 Hz, 1H), 6.93-6.96 (m, 2H), 6.99-7.03 (m, 2H), 7.07-7.11 (m, 2H), 7.22-7.24 (m, 2H), 7.27-7.29 (m, 3H), 7.32-7.36 (dd, J=7.82, 4.40 Hz, 2H), 7.52-7.53 (d, J=7.82 Hz, 1H)

(S)—N-(3-(1H-indol-3-yl)-1-((4-(4-methoxyphenyl)thiazol-2-yl)amino)-1-oxopropan-2-yl)-4-methylbenzamide

[0535] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 2.33 (s, 3H), 3.23-3.34 (m, 2H), 3.78 (s, 3H), 4.95-4.99 (m, 1H), 6.97-7.00 (m, 3H), 7.04-7.07 (t, J=7.82 Hz, 1H), 7.24-7.26 (d, J=7.82 Hz, 2H), 7.30-7.32 (m, 2H), 7.45 (s, 1H), 7.73-7.75 (d, J=7.82 Hz, 2H), 7.83-7.84 (d, J=8.80 Hz, 3H), 8.62-8.63 (d, J=7.82 Hz, 1H), 10.84 (s, 1H), 12.64 (s, 1H)

(S)-2-(4-Chlorophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide

[0536] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 2.86-2.91 (dd, J=14.18, 8.80 Hz, 1H), 3.08-3.12 (dd, J=14.67, 6.35 Hz, 1H), 3.78 (s, 3H), 4.33 (brs, 1H), 6.90-6.93 (t, J=7.33 Hz, 1H), 6.97-6.99 (d, J=8.80 Hz, 2H), 7.02-7.05 (t, J=7.33 Hz, 1H), 7.08 (d, J=1.95 Hz, 1H), 7.22-7.24 (d, J=8.80 Hz, 2H), 7.26-7.27 (d, J=8.31 Hz, 1H), 7.43 (s, 1H), 7.46-7.48 (d, J=8.80 Hz, 3H), 7.79-7.81 (d, J=8.80 Hz, 2H), 8.50 (brs, 1H), 10.78 (s, 1H), 12.44 (brs, 1H)

(S)-3-(1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-2-(4-(trifluoromethyl)phenylsulfonamido)propanamide

[0537] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 2.88-2.93 (dd, J=14.67, 9.29 Hz, 1H), 3.09-3.13 (dd, J=14.18, 5.18 Hz, 1H), 3.78 (s, 3H), 4.37 (brs, 1H), 6.88-6.91 (t, J=7.33 Hz, 1H), 6.97-7.02 (m, 3H), 7.10 (d, J=1.95 Hz, 1H), 7.22-7.24 (d, J=8.31 Hz, 1H), 7.42 (s, 1H), 7.48-7.53 (m, 3H), 7.65-7.67 (d, J=7.82 Hz, 2H), 7.79-7.80 (d, J=8.31 Hz, 2H), 8.70 (brs, 1H), 10.77 (s, 1H), 12.46 (brs, 1H)

(S)-2-(4-Fluorophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide

[0538] .sup.1H-NMR (500 MHz, CD.sub.3OD) δ 2.87-2.92 (dd, J=14.67, 8.80, Hz, 1H), 3.08-3.12 (dd, J=14.18, 6.35 Hz, 1H), 3.76 (s, 3H), 4.28-4.31 (dd, J=8.31, 6.84 Hz, 1H), 6.89-6.92 (m, 1H), 6.96-7.06 (m, 4H), 7.08 (s, 1H), 7.26-7.28 (m, 1H), 7.39 (s, 1H), 7.46-7.47 (d, J=7.82 Hz, 1H), 7.54-7.58 (m, 2H), 7.78-7.81 (m, 2H), 10.82 (brs, 1H)

(S)-2-(4-Bromophenylsulfonamido)-N-((1r,3R,5S,7S)-3,5-dimethyladamantan-1-yl)-3-(1H-indol-3-yl)propanamide

[0539] .sup.1H-NMR (500 MHz, CDCl.sub.3) δ 0.80 (s, 6H), 1.08 (s, 2H), 1.22-1.43 (m, 8H), 1.59 (s, 2H), 2.07 (s, 1H), 3.03-3.07 (dd, J=14.67, 7.33 Hz, 1H), 3.16-3.20 (dd, J=14.67, 6.84 Hz, 1H), 3.77-3.80 (m, 1H), 5.36-5.37 (d, J=6.35 Hz, 1H), 5.70 (s, 1H), 6.97 (s, 1H), 7.03-7.06 (t, J=7.33 Hz, 1H), 7.20-7.23 (t, J=7.33 Hz, 1H), 7.32-7.38 (m, 4H), 7.63-7.64 (d, J=8.80 Hz, 1H), 7.77-7.79 (d, J=8.31 Hz, 1H), 8.20 (s, 1H)

(S)-2-(4-Cyanophenylsulfonamido)-3-(1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide

[0540] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 2.85-2.90 (dd, J=14.67, 9.78 Hz, 1H), 3.05-3.09 (dd, J=14.18, 5.38 Hz, 1H), 3.78 (s, 3H), 4.34 (brs, 1H), 6.89-6.92 (t, J=7.82 Hz, 1H), 6.98-7.04 (m, 3H), 7.07-7.08 (d, J=1.95 Hz, 1H), 7.22-7.23 (d, J=8.31 Hz, 1H), 7.46-7.52 (m, 6H), 7.82-7.83 (d, J=8.80 Hz, 2H), 8.74 (brs, 1H), 10.72-10.72 (d, J=1.46 Hz, 1H), 12.58 (brs, 1H)

(S)-Benzyl 3-(1H-indol-3-yl)-2-(4-methylbenzamido)propanoate

[0541] .sup.1H-NMR (500 MHz, CDCl.sub.3) δ 3.36-3.43 (m, 2H), 5.03-5.10 (m, 2H), 5.15-5.18 (dt, J=7.82, 5.38×2 Hz, 1H), 6.69-6.70 (d, J=2.44 Hz, 1H), 6.76-6.78 (d, J=7.82 Hz, 1H), 7.01-7.04 (t, J=7.33 Hz, 1H), 7.07-7.08 (d, J=8.31 Hz, 2H), 7.10-7.13 (t, J=7.33 Hz, 1H), 7.21-7.31 (m, 6H), 7.50-7.51 (d, J=7.82 Hz, 1H), 7.53-7.54 (d, J=8.31 Hz, 2H), 8.64 (brs, 1H)

(S)-2-(4-Bromophenylsulfonamido)-3-(5-hydroxy-1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide

[0542] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 2.79-2.83 (dd, J=14.18, 8.31 Hz, 1H), 2.99-3.03 (dd, J=14.18, 6.84 Hz, 1H), 3.77 (s, 3H), 4.31-4.34 (q, J=8.31, 7.82, 7.33 Hz, 1H), 6.58-6.60 (dd, J=8.80, 2.44 Hz, 1H), 6.86 (d, J=1.95 Hz, 1H), 6.97-6.99 (m, 3H), 7.06-7.07 (d, J=8.80 Hz, 1H), 7.40-7.46 (m, 4H), 7.77-7.84 (m, 2H), 8.46-8.48 (d, J=8.31 Hz, 1H), 8.61 (brs, 1H), 10.47-10.48 (d, J=1.95 Hz, 1H), 12.4 (s, 1H)

(S)-2-(4-Bromophenylsulfonamido)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-3-(5-methyl-1H-indol-3-yl)propanamide

[0543] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 2.33 (s, 3H), 2.82-2.86 (dd, J=14.18, 8.31 Hz, 1H), 3.04-3.09 (dd, J=14.67, 6.84 Hz, 1H), 3.77 (s, 3H), 4.29 (brs, 1H), 6.84-6.86 (d, J=8.31 Hz, 1H), 6.97-7.02 (m, 3H), 7.14-7.16 (m, 2H), 7.41-7.45 (m, 5H), 7.79-7.81 (d, J=8.31 Hz, 2H), 8.47 (brs, 1H), 10.64 (s, 1H), 12.40 (brs, 1H)

(S)-2-(4-Bromophenylsulfonamido)-3-(5-fluoro-1H-indol-3-yl)-N-(4-(4-methoxyphenyl)thiazol-2-yl)propanamide

[0544] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 2.97-3.02 (dd, J=14.18, 8.80 Hz, 1H), 3.17-3.22 (dd, J=14.18, 5.86 Hz, 1H), 3.81 (s, 3H), 4.24-4.27 (dd, J=8.80, 6.35 Hz, 1H), 4.62 (s, 1H), 6.81-6.85 (td, J=9.29×2, 2.44 Hz, 1H), 6.92-6.94 (d, J=8.80 Hz, 2H), 7.08 (s, 1H), 7.12-7.14 (dd, J=10.27, 1.95 Hz, 1H), 7.17 (s, 1H), 7.21-7.22 (dd, J=8.80, 4.40 Hz, 1H), 7.27-7.29 (d, J=8.31 Hz, 2H), 7.41-7.43 (d, J=8.31 Hz, 2H), 7.77-7.79 (d, J=8.31 Hz, 2H)

(S)-4-(2-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)ethyl)benzoic acid

[0545] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 2.28 (s, 3H), 2.54-2.64 (m, 2H), 2.80-2.85 (dd, J=14.18, 7.82 Hz, 1H), 3.09-3.20 (m, 2H), 3.26-3.30 (dd, J=13.20, 6.35 Hz, 1H), 3.86-3.89 (dd, J=7.82, 6.35 Hz, 1H), 6.90-6.93 (t, J=7.82 Hz, 1H), 6.95 (s, 1H), 7.00-7.02 (d, J=8.31 Hz, 2H), 7.04-7.07 (t, J=6.84 Hz, 1H), 7.14-7.15 (d, J=8.31 Hz, 2H), 7.26-7.27 (d, J=7.82 Hz, 1H), 7.31-7.32 (d, J=7.82 Hz, 1H), 7.40-7.41 (d, J=8.31 Hz, 2H), 7.90-7.91 (d, J=7.82 Hz, 3H), 10.22 (s, 1H)

(S)—N-(4-bromophenethyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide

[0546] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 2.27 (s, 3H), 2.36-2.43 (m, 2H), 2.69-2.73 (dd, J=14.18, 7.82 Hz, 1H), 2.88-2.98 (m, 2H), 3.03-3.08 (dt, J=13.20, 6.84, 6.35 Hz, 1H), 3.82-3.85 (t, J=6.84 Hz, 1H), 6.89-6.92 (t, J=7.33 Hz, 1H), 6.97-6.99 (d, 8.31 Hz, 2H), 7.01-7.04 (t, J=7.33 Hz, 2H), 7.12-7.14 (d, J=8.31 Hz, 2H), 7.28-7.32 (dd, J=11.24, 8.31 Hz, 2H), 7.37-7.39 (d, J=7.33 Hz, 2H), 7.44-7.46 (d, J=7.82 Hz, 2H), 7.91-7.93 (t, J=5.38 Hz, 2H), 10.75 (brs, 1H)

(S)—N-(2-(1H-indol-3-yl)ethyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide

[0547] .sup.1H-NMR (500 Mz, CD.sub.3OD) δ 2.24 (s, 3H), 2.64-2.76 (m, 2H), 2.82-2.86 (dd, J=14.67, 8.31 Hz, 1H), 3.11-3.15 (dd, J=14.67, 5.86 Hz, 1H), 3.20-3.26 (m, 1H), 3.30-3.36 (m, 1H), 3.89-3.91 (dd, J=8.31, 6.35 Hz, 1H), 6.91-7.01 (m, 6H), 7.04-7.10 (m, 2H), 7.25-7.27 (d, J=7.82 Hz, 1H), 7.32-7.35 (m, 2H), 7.36-7.38 (d, J=8.31 Hz, 2H), 7.48-7.49 (d, J=7.82 Hz, 1H)

(S)-3-(1H-indol-3-yl)-N-(4-methylphenethyl)-2-(4-methylphenylsulfonamido)propanamide

[0548] .sup.1H-NMR (500 MHz, CD.sub.3OD) δ 2.27-2.27 (d, J=4.89 Hz, 6H), 2.43-2.54 (m, 2H), 2.80-2.85 (dd, J=14.18, 8.13 Hz, 1H), 3.07-3.14 (m, 2H), 3.21-3.26 (m, 1H), 3.86-3.89 (t, J=6.84 Hz, 1H), 6.91-7.07 (m, 9H), 7.25-7.27 (d, J=7.82 Hz, 1H), 7.32-7.33 (d, J=7.82 Hz, 1H), 7.40-7.41 (d, J=7.82 Hz, 2H)

Ethyl 2-((S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)-3-(1H-indol-3-yl)propanoate

[0549] .sup.1H-NMR (500 MHz, CD.sub.3OD) δ 1.07-1.10 (t, J=7.33 Hz, 3H), 2.18 (s, 3H), 2.80-2.85 (dd, J=14.67, 8.80 Hz, 1H), 3.06-3.18 (m, 3H), 3.97-4.05 (m, 3H), 4.53-4.55 (t, J=6.84 Hz, 1H), 6.82-6.84 (d, J=7.82 Hz, 2H), 6.90-6.94 (m, 1H), 6.96 (s, 1H), 7.00-7.06 (m, 3H), 7.10-7.13 (td, J=7.82, 7.33 Hz, 1H), 7.24-7.26 (d, J=7.82 Hz, 1H), 7.29-7.30 (d, J=8.31 Hz, 2H), 7.34-7.36 (dt, J=8.31×2 Hz, 2H), 7.45-7.46 (d, J=7.82 Hz, 1H)

(S)—N-(4-chlorophenethyl)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamide

[0550] .sup.1H-NMR (500 MHz, CD.sub.3OD) δ 2.29 (s, 3H), 2.46-2.57 (m, 2H), 2.80-2.84 (dd, J=14.18, 7.82 Hz, 1H), 3.07-3.14 (m, 2H), 3.24-3.29 (m, 1H), 3.86-3.89 (t, J=6.35 Hz, 1H), 6.91-6.96 (m, 2H), 7.02-7.08 (m, 5H), 7.19-7.21 (d, J=8.31 Hz, 2H), 7.26-7.28 (d, J=7.82 Hz, 1H), 7.31-7.33 (d, J=7.82 Hz, 1H), 7.41-7.42 (d, J=7.82 Hz, 2H)

2-((S)-3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)-3-(1H-Indol-3-yl)propanoic acid

[0551] .sup.1H-NMR (500 MHz, CD.sub.3OD) δ 2.18 (s, 3H), 2.57-2.62 (dd, J=14.67, 10.27, Hz, 1H), 3.12-3.21 (dd, J=14.67, 3.42 Hz, 1H), 3.21-3.25 (dd, J=14.67, 6.35 Hz, 1H), 3.37-3.41 (dd, J=14.67, 4.89 Hz, 1H), 3.87-3.89 (dd, J=9.78, 3.91 Hz, 1H), 4.51-4.53 (t, J=5.86 Hz, 1H), 6.72-6.74 (d, J=8.31 Hz, 2H), 6.84 (s, 1H), 6.86-6.89 (t, J=7.82 Hz, 1H), 6.97-7.00 (t, J=7.82 Hz, 1H), 7.02-7.09 (m, 2H), 7.13-7.15 (m, 3H), 7.20-7.21 (d, J=7.82 Hz, 1H), 7.29-7.32 (dd, J=7.33, 6.84 Hz, 2H), 7.59-7.61 (d, J=7.82 Hz, 1H)

(S)-Methyl 4-(2-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)thiazol-4-yl)benzoate

[0552] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 2.16 (s, 3H), 2.49-2.50 (dd, J=14.18, 7.82, 6.35 Hz, 1H), 3.07-3.11 (dd, J=14.18, 7.33, 6.84 Hz, 1H), 3.85 (s, 3H), 4.30 (brs, 1H), 6.89-6.92 (t, J=7.33 Hz, 1H), 7.01-7.07 (m, 4H), 7.26-7.28 (d, J=7.82 Hz, 1H), 7.41-7.42 (d, J=7.82 Hz, 1H), 7.45-7.47 (d, J=8.31 Hz, 2H), 7.80 (s, 1H), 8.01 (s, 4H), 8.27 (brs, 1H), 10.79 (s, 1H), 12.41 (brs, 1H)

(S)-4-(2-(3-(1H-indol-3-yl)-2-(4-methylphenylsulfonamido)propanamido)thiazol-4-yl)benzoic acid

[0553] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 2.18 (s, 3H), 2.87-2.91 (dd. J=14.18, 7.82 Hz, 1H), 3.09-3.13 (dd, J=14.18, 6.84 Hz, 1H), 4.31-4.36 (q, J=7.82×3 Hz, 1H), 6.91-6.94 (t, J=7.33 Hz, 1H), 7.03-7.09 (m, 4H), 7.28-7.30 (d, J=7.82 Hz, 1H), 7.43-7.44 (d, J=7.82 Hz, 1H), 7.47-7.49 (d, J=7.82 Hz, 2H), 7.80 (s, 1H), 7.99-8.03 (m, 4H), 8.28-8.30 (d, J=8.80 Hz, 1H), 10.81 (s, 1H), 12.43 (s, 1H), 12.98 (brs, 1H)

(S)-3-(Benzo[d]oxazol-2-ylamino)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-2-(4-methylphenylsulfonamido)propanamide

[0554] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 2.13 (s, 3H), 3.51-3.55 (m, 2H), 3.79 (s, 3H), 4.35-4.36 (d, J=5.38 Hz, 1H), 6.98-7.01 (m, 3H), 7.11-7.15 (m, 3H), 7.22-7.24 (d, J=7.82 Hz, 1H), 7.30-7.32 (d, J=7.82 Hz, 1H), 7.44 (s, 1H), 7.65-7.66 (d, J=8.31 Hz, 2H), 7.80-7.82 (d, J=8.31 Hz, 2H), 7.99-8.01 (t, J=6.35 Hz, 1H), 8.20-8.21 (d, J=5.86 Hz, 1H), 12.33 (brs, 1H)

(S)—N-(3-((4-(4-methoxyphenyl)thiazol-2-yl)amino)-2-(4-methylphenylsulfonamido)-3-oxopropyl)benzamide

[0555] .sup.1H-NMR (500 MHz, CD.sub.3OD) δ 2.20 (s, 3H), 3.63-3.67 (m, 1H), 3.73-3.75 (m, 1H), 3.88 (s, 3H), 4.33-4.35 (t, J=6.35 Hz, 1H), 6.99-7.01 (d, J=8.80 Hz, 2H), 7.17-7.18 (d, J=7.82 Hz, 2H), 7.24 (s, 1H), 7.47-7.50 (m, 2H), 7.57-7.60 (m, 1H), 7.74-7.78 (dd, J=14.18, 7.82 Hz, 4H), 7.85-7.86 (d, J=8.31 Hz, 2H)

(S)—N-(3-((4-(4-methoxyphenyl)thiazol-2-yl)amino)-2-(4-methylphenylsulfonamido)-3-oxopropyl)nicotinamide

[0556] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 2.14 (s, 3H), 3.48-3.53 (dt, J=13.20, 6.84, 6.35 Hz, 1H), 3.56-3.63 (m, 1H), 3.78 (s, 3H), 4.23-4.26 (t, J=6.84 Hz, 1H), 6.97-6.99 (d, J=8.80 Hz, 2H), 7.14-7.16 (d, J=8.31 Hz, 2H), 7.42 (s, 1H), 7.45-7.48 (dd, J=7.82, 4.89, 2.93 Hz, 1H), 7.64-7.66 (d, J=8.31 Hz, 2H), 7.79-7.80 (d, J=8.80 Hz, 2H), 8.01-8.03 (dt, J=7.82, 1.95×2 Hz, 1H), 8.11 (brs, 1H), 8.65-8.68 (m, 2H), 8.84-8.85 (d, J=1.46 Hz, 1H), 12.28 (brs, 1H)

(S)—N-(3-((4-(4-methoxyphenyl)thiazol-2-yl)amino)-2-(4-methylphenylsulfonamido)-3-oxopropyl)pyrimidine-5-carboxamide

[0557] .sup.1H-NMR (500 MHz, DMSO-d.sub.6) δ 2.16 (s, 3H), 3.49-3.53 (dt, J=13.69, 6.84×2 Hz, 1H), 3.57-3.63 (dt, J=13.20, 6.35×2 Hz, 1H), 3.79 (s, 3H), 4.23-4.26 (m, 1H), 6.98-7.00 (d, J=8.80 Hz, 2H), 7.17-7.19 (d, J=8.31 Hz, 2H), 7.45 (s, 1H), 7.65-7.67 (d, J=8.31 Hz, 2H), 7.79-7.81 (d, J=8.80 Hz, 2H), 8.18-8.19 (d, J=7.82 Hz, 1H), 8.87-8.89 (t, J=5.86 Hz, 1H), 9.00 (s, 2H), 9.31 (s, 1H), 12.31 (brs, 1H)

Example 2: DX2-Nanoluciferase Activity (40 uM) and Cell Viability (% Inhibition)

[0558] After cloning DX2 into a plasmid expressing nanoluciferase, the plasmid was transfected into A549 cells. Transfected cells were seeded 1×10.sup.4 per well in a 96-well plate and stabilized for 12 hours. The compound was treated for 4 hours, and then the expression change of DX2 could be observed through luciferase assay. Cell viability was measured by the MTT method after 72 hours of treatment with each concentration of the compound in A549 cells.

[0559] The results are shown in Table 1 above.

Example 3: AIMP2-DX2 and AIMP2 Inhibition Evaluation (Nanoluciferase Assay)

[0560] Compound No. 63 was selected from among the compounds showing excellent effects in Table 1, and the following experiment was performed.

[0561] In order to calculate the IC50 of compound No. 63, A549 cells expressing nanoluciferase-DX2 or -AIMP2 were treated with compound No. 63 at each concentration for 4 hours, and then fluorescence was measured.

[0562] The results for this are shown in FIG. 1.

[0563] As shown in FIG. 1, it was confirmed that the inhibition rate for AIMP2-DX2 and AIMP2 of compound No. 63 shows 100-fold or more selectivity for AIMP2-DX2 (DX2 IC50-0.92 μM and AIMP2 IC50 >100 μM).

Example 4: AIMP2-DX2 Inhibition Mechanism Study

[0564] As previously reported, AIMP2-DX2 is stabilized by binding to HSP70. Therefore, the present inventors checked whether the compound No. 63, which showed the best AIMP2-DX2 inhibitory ability, can inhibit the binding of AIMP2-DX2 and HSP70. Specifically, an in vitro pull-down assay was performed in the presence of compound No. 63 using purified AIMP2-DX2 and HSP70 protein.

[0565] The results for this are shown in FIG. 2.

[0566] As shown in FIG. 2, it was confirmed that compound No. 63 inhibited the binding of AIMP2-DX2 and HSP70 in a concentration-dependent manner.

Example 5: In Vivo Anti-Cancer Efficacy Evaluation

[0567] Next, the anti-cancer efficacy of compound No. 63 was evaluated in a mouse model transplanted with H460 cells.

[0568] Specifically, the compound No. 63 was intraperitoneally administered to mice transplanted with H460 cells at 50 mg/kg, once every two days for a total of 15 days.

[0569] The results are shown in FIGS. 3a to 3d.

[0570] As shown in FIGS. 3a to 3d, compound No. 63 significantly inhibited the growth of tumors, and it was confirmed that there was no change in the body weight of the animals during the administration period.

Example 6: Inhibitory Effect of Compound No. 55 and Compound No. 89 on Cancer Growth In Vivo

[0571] Additionally, compounds No. 55 and No. 88 were selected from Table 1, and an in vivo cancer growth inhibitory effect experiment was performed.

[0572] H460 cells (2×10.sup.7) were subcutaneously implanted in 7-week-old BALB/cAnCr female rats, and then Compound No. 55 or Compound No. 89 (50 mg/kg) and Taxol (10 mg/kg) were administered intraperitoneally once every 2 days. The drug was administered for 16 days, and the size of the tumor and the weight of the animal were measured during administration. After 16 days, the animals were sacrificed and the size and weight of the removed tumors were measured.

[0573] The results for this are shown in FIG. 4.

[0574] At the treated concentration, compound No. 55 showed about 50% cancer growth inhibitory effect during the treatment period, and it is judged that there is no side effect of the compound as there is no change in the body weight of the animal during the treatment period.

INDUSTRIAL APPLICABILITY

[0575] The compound represented by Formula 1 according to the present invention is very effective in inhibiting the expression of AIMP2-DX2, so it can be very usefully used in the development of various diseases caused by AIMP2-DX2, in particular, a therapeutic agent for cancer.