AROMATIC SULPHONAMIDES DERIVATIVES THAT INHIBITS PDI A3, THEIR SYNTHESIS AND USE

Abstract

The invention relates to a new group of aromatic sulphonamides derivatives of formula (I) and their synthesis and use for modulation of the activity of protein disulfide isomerase (PDI). More particularly, the invention provides small molecule inhibitors of PDI A1 that display antiplatelet, antithrombotic and anticancer activities.

Claims

1. N,N-disubstituted aromatic sulphonamides of formula (I) in form of racemates or enantiomers that inhibits PDI A1: ##STR00028## or a pharmaceutically acceptable salt and/or prodrug, wherein R.sup.1 and R.sup.2 taken together represent group of substituents consisting of formula (II) ##STR00029## wherein R.sup.6 represents CN, CONR.sup.7R.sup.8, COOR.sup.9, COO.sup.-Met.sup.+, COR.sup.10, ##STR00030## wherein: R.sup.7 and R.sup.8 independently represent H or lower alkyl C.sub.1-C.sub.4, R.sup.9 and R.sup.10 independently represent lower alkyl C1-C4; Met.sup.+ independently represent an alkali metal cation Li.sup.+, Na.sup.+ or K.sup.+ and wherein Aryl- represents: mono, di- and tri-substituted phenyl group of formula (III): ##STR00031## wherein R.sup.3, R.sup.4 and R.sup.5 independently represent selected from group of substituents, consisting of: H, linear alkyl group C.sub.1-C.sub.12, O-alkyl C.sub.1-C.sub.4, branched alkyl C.sub.3-C.sub.4, cycloalkyl, phenyl, NO.sub.2, halogen (Cl, F), trifluoromethyl, lower C.sub.1-C.sub.4 alkoxy, lower C.sub.1-C.sub.4 dialkylamino, lower C.sub.1-C.sub.4 acylamino, unsubstituted-, mono- and di- substituted- α -, β- and γ-naphthy1-group of formula IV : ##STR00032## wherein R.sup.15, R.sup.16 and R.sup.17 independently represent H, lower alkyl C.sub.1-C.sub.4, Cl, O-alkyl C.sub.1-C.sub.4, -CHO and NR.sup.18R.sup.19, where R.sup.18 and R.sup.19 are H or lower alkyl C.sub.1-C.sub.4, pyridin-3-yl group of formula V: ##STR00033## or 2-oxochromen-6-yl group of formula VI: ##STR00034## or 2-oxo-1H-quinolin-6-y1group of formula VII: ##STR00035## with the exception that the compound is not selected from the group comprising Methyl 1-(p-tolylsulfonyl)aziridine-2-carboxylate (C-3161), Methyl 1-(4-nitropheny1)sulfonylaziridine-2-carboxylate (C-3212), 1-(p-Tolylsulfonyl)aziridine-2-carboxamide (C-3220), Methyl 1-(benzenesulfonyl)aziridine-2-carboxylate (C-3251), 1-(p-Tolylsulfonyl)aziridine-2-carbaldehyde (C-3262), 1-[1-(p-Tolylsulfonyl)aziridin-2-yl]ethanone (C-3263), Methyl 1-(4-chloropheny1)sulfony1aziridine-2-carboxylate (C-3296), Methyl 1-(4-propylpheny1)sulfonylaziridine-2-carboxylate (C-3304), 1-(p-Tolylsulfonyl)aziridine-2-carbonitrile (C-3314), N,N-Dimethyl-1-(p-tolylsulfonyl)aziridine-2-carboxamide (C-3342).

2. N,N-disubstituted aromatic sulphonamides according to claim 1, wherein the compounds are chosen for the list: 1 -(4-Hexylphenyl)sulfonylaziridine-2-carboxamide (C-3389) 1-(4-Heaylphenyl)sulfonyl-N-methyl-aziridine-2-carboxamide (C-3380) 1-(4-Heaylphenyl)sulfonyl-N,N-dimethyl-aziridine-2-carboxamide (C-3369) Methyl l-(4-hexylphenyl)sulfonylaziridine-2-carboxylate (C-3287) Methyl l-(4-butylphenyl)sulfonylaziridine-2-carboxylate (C-3257) N,N-Dimethyl-1-(4-pentylphenyl)sulfonyl-aziridine-2-carboxamide (C-3368) Methyl l-[[5-(dimethylamino)-2-naphthyl]sulfonyl]aziridine-2-carboxylate (C-3399) 1 -(4-Cyclohexylphenyl)sulfonyl-N,N-dimethyl-aziridine-2-carboxamide (C-3384) Methyl l-(4-pentylphenyl)sulfonylaziridine-2-carboxylate (C-3281) Methyl 1 -[[6-(dimethylamino)-5-formy1-1 -naphthy1] sulfony1]aziridine-2-carboxylate (C-3376) 1-[[5-(Dimethylamino)-2-naphthyl]sulfonyl]-N,N-dimethylaziridine-2-carboxamide (C-3400) Methyl 1 -[[4-(dimethylamino)-1 -naphthy1] sulfonyl]aziridine-2-carboxylate (C-3383) 1-[[6-(Dimethylamino)-1-naphthyl]sulfonyl]-N,N-dimethylaziridine-2-carboxamide (C-3377) Methyl 1 -[[6-(dimethylamino)-1 -naphthy1] sulfonyl]aziridine-2-carboxylate (C-3375) Methyl l-[[5-chloro-6-(methylamino)-2-naphthyl]sulfonyl]aziridine-2-carboxylate (C-3393) 1-[[6-(Dimethylamino)-5-formyl-2-naphthyl]sulfonyl]-N,N-dimethylaziridine-2-carboxamide (C-3391) Methyl 1-(4-isopropylphenyl)sulfonylaziridine-2-carboaylate (C-3295) Methyl l-(4-tert-butylphenyl)sulfonylaziridine-2-carboxylate (C-3290) Methyl 1-(4-phenylphenyl)sulfonylaziridine-2-carboaylate (C-3291) Methyl l-(4-heptylphenyl)sulfonylaziridine-2-carboxylate (C-3288) 1-[[5-(Dimethylamino)-1-naphthyl]sulfonyl]-N,N-dimethylaziridine-2-carboxamide (C-3371) l-(4-Butylphenyl)sulfonyl-N,N-dimethyl-aziridine-2-carboxamide (C-3362) 1-[1-(4-Butylphenyl)sulfonylaziridin-2-yl]ethanone (C-3272) Methyl 1-(2-naphthylsulfonyl)aziridine-2-carboaylate (C-3292) Methyl 1-[4-(trifluoromethyl)phenyl]sulfonylaziridine-2-carboaylate (C-3256) Methyl 1-(2-fluoro-4-methyl-phenyl)sulfonylaziridine-2-carboaylate (C-3397) Methyl 1-[[6-(dimethylamino)-5-formyl-2-naphthyl]sulfonyl]aziridine-2-carboaylate (C-3390).

3. Method for the preparation of N,N-disubstituted aromatic sulphonamides derivatives of claim 1, wherein: solution of appropriate aziridine derivative of formula VIII or its enantiomer ##STR00036## wherein R.sup.6 represents: CN, CONR.sup.7R.sup.8, COOR.sup.9, COO.sup.-Met.sup.+, COR.sub.10,, ##STR00037## wherein: R.sup.7 and R.sup.8 are H or lower alkyl C.sub.1-C.sub.4, and R.sup.9 and R.sup.10 is lower alkyl C1-C4; in presence of base is treated with appropriate sufonylchloride of formula IX ##STR00038## which is selected from group of aryl-sulfonylchloride, wherein Aryl- independently represent: mono, di- and tri-substituted phenyl group of formula (III): ##STR00039## wherein R.sup.3, R.sup.4 and R.sup.5 independently represent selected from group of substituents, consisting of: H, linear alkyl group C.sub.1-C.sub.12, O-alkyl C.sub.1-C.sub.4, branched alkyl C.sub.3-C.sub.4, cycloalkyl, phenyl, NO.sub.2, halogen (Cl, F), trifluoromethyl, lower C.sub.1-C.sub.4 alkoxy, lower C.sub.1-C.sub.4 dialkylamino, lower C.sub.1-C.sub.4 acylamino; or Aryl- represents unsubstituted-, mono- and di- substituted- α -, β- and γ-naphthy1-group of formula IV : ##STR00040## wherein R.sup.15, R.sup.16 and R.sup.17 are selected form group consisting of H, lower alkyl C.sub.1-C.sub.4, Cl, O-alkyl C.sub.1-C.sub.4, -CHO and NR.sup.18R.sup.19, where R.sup.18 and R.sup.19 are H or lower alkyl C1-C4; or pyridin-3-yl group of formula V: ##STR00041## or 2-oxochromen-6-yl group of formula VI: ##STR00042## or 2-oxo-1H-quinolin-6-y1group of formula VII: ##STR00043## .

4. N,N-disubstituted aromatic sulphonamides of formula (I) that inhibits PDI A1 ##STR00044## or a pharmaceutically acceptable salt and/or prodrug, wherein: R.sup.1 and R.sup.2 taken together represent group of substituents consisting of formula (II) ##STR00045## wherein R.sup.6 represents: CN, CONR.sup.7R.sup.8, COOR.sup.9, COO.sup.-Met.sup.+, COR.sup.10, ##STR00046## wherein: R.sup.7 and R.sup.8 independently represent H or lower alkyl C.sub.1-C.sub.4, R.sup.9 and R.sup.10 independently represent lower alkyl C1-C4; Met.sup.+ represents an alkali metal cation Li.sup.+, Na.sup.+ or K.sup.+and wherein Aryl- represents mono, di- and tri-substituted phenyl group of formula (III): ##STR00047## wherein R.sup.3, R.sup.4 and R.sup.5 independently represent H, linear alkyl group C.sub.1-C.sub.12, O-alkyl C.sub.1-C.sub.4, branched alkyl C.sub.3-C.sub.4, cycloalkyl, phenyl, NO.sub.2, halogen (Cl, F), trifluoromethyl, lower C.sub.1-C.sub.4 alkoxy, lower C.sub.1-C.sub.4 dialkylamino, lower C.sub.1-C.sub.4 acylamino group, or wherein Aryl- represents unsubstituted-, mono- and di- substituted- α -, β- and γ-naphthy1-group of formula IV : ##STR00048## wherein R.sup.15, R.sup.16 and R.sup.17 independently represent: H, lower alkyl C.sub.1-C.sub.4, Cl, O-alkyl C.sub.1-C.sub.4, -CHO and NR.sup.18R.sup.19 , whereoin R.sup.18 and R.sup.19 independently represent H, lower alkyl C1-C4; or wherein Aryl- represents pyridin-3-yl group of formula V: ##STR00049## or 2-oxochromen-6-yl group of formula VI: ##STR00050## and 2-oxo-1H-quinolin-6-y1group of formula VII: ##STR00051## for use as a medicament.

5. N,N-disubstituted aromatic sulphonamides according to claim 4, for use in treatment and prevention of excessive platelet activation and thrombosis, in particular any disease from the list: disease or condition is thrombosis, thrombotic diseases, in particular the thrombotic disease is acute myocardial infarction, stable angina, unstable angina, aortocoronary bypass surgery, acute occlusion following coronary angioplasty and/or stent placement, transient ischemic attacks, cerebrovascular disease, peripheral vascular disease, placental insufficiency, prosthetic heart valves, atrial fibrillation, anticoagulation of tubing, deep vein thrombosis or pulmonary embolism and other pathologies linked with excessive activation of platelets.

6. N,N-disubstituted aromatic sulphonamides according to claim 4, for use in treatment and prevention of cancer, in particular any disease from the list: gastrointestinal cancer, colorectal cancer, colon cancer, liver cancer, hepatocellular carcinoma, pancreatic cancer, biliary tract cancer, stomach cancer, genitourinary cancer, bladder cancer, testicular cancer, cervical cancer, malignant mesothelioma, osteogenic sarcoma, esophageal cancer, laryngeal cancer, prostate cancer, hormone-refractory prostate cancer, lung cancer, small cell lung cancer, non-small cell lung cancer, breast cancer, triple-negative breast cancer, breast cancer having a BRCA1 and/or BRCA2 gene mutation, hematological cancer, leukemia, acute lymphoblastic leukemia, acute myeloid leukemia, chronic lymphocytic leukemia, chronic myeloid leukemia, lymphoma, Hodgkin lymphoma, non-Hodgkin lymphoma, follicular lymphoma, diffuse large B-cell lymphoma, ovarian cancer, brain cancer, neuroblastoma, Ewing’s sarcoma, kidney cancer, epidermoid cancer, skin cancer, melanoma, head and/or neck cancer, head and neck squamous cell carcinoma, and mouth cancer.

Description

[0066] The invention has been described in embodiments and figures non-limiting of the scope of protection, where:

[0067] FIG. 1 shows the influence of PDI A1 inhibitor C-3251 on the clonogenic potential, cell cycle and cell death of human colon cancer cell lines;

[0068] FIG. 2 shows effect of bepristat and C-3380 and C-3389 inhibitor on MDA-MB-231 cell transendothelial migration across endothelial monolayer;

[0069] FIG. 3 shows antiplatelet antithrombotic effects in in vivo model of thrombosis for selected PDI A1 inhibitor and reference compounds;

[0070] FIG. 4 shows dose dependence of the anti-thrombotic effects for the selected PDIA1 inhibitor in in vivo model of thrombosis.

[0071] FIGS. 5, 6 show anti-cancer activity of selected PDI-inhibitors in vivo

EXAMPLE 1. CHEMICAL SYNTHESIS

[0072] It is described below the general method for the preparation of the aziridine aromatic N-sulphonamides of formula (I).

##STR00021##

X=COOAlkyl, CONH.sub.2, CONHAlkyl, CONAlkyl.sub.2,CN, CHO, COAlkyl ,

##STR00022##

##STR00023##

##STR00024##

wherein R.sup.3, R.sup.4 and R.sup.5 are: H, linear alkyl group C.sub.1-C.sub.12, O-alkyl C.sub.1-C.sub.4, branched alkyl C.sub.3-C.sub.4, cycloalkyl, phenyl, NO.sub.2, halogen (Cl, F), trifluoromethyl, lower C.sub.1-C.sub.4 alkoxy, lower C.sub.1-C.sub.4 dialkylamino, lower C.sub.1-C.sub.4 acylamino; and R.sup.15, R.sup.16, R.sup.17 are: H, lower alkyl C.sub.1-C.sub.4, Cl, O-alkyl C.sub.1-C.sub.4, -CHO and NR.sup.18R.sup.19 , where R.sup.18 and R.sup.19 are H or lower alkyl C.sub.1-C.sub.4

[0073] Aromatic or heteroaromatic sulphonic acid chloride (1 mmol) was added with stirring to the solution of the corresponding aziridine (1.1 mmol) and K.sub.2CO.sub.3 (2 mmol) in the mixture of 1 ml CHCl.sub.3 + 1 ml water. The mixture was stirred for 24 h. at room temperature. Product was extracted with CHCl.sub.3, and the solution dried over MgSO.sub.4. The solvent was evaporated. The product was purified by chromatography (silica gel, petroleum ether/ethyl acetate 4:1=>1:2) to give corresponding aziridine aromatic N-sulfonamide.

[0074] 1-(p-Tolylsulfonyl)aziridine-2-carbonitrile (C-3314) was prepared as described by Nadir, U. K. and Singh, A. Synthetic Communications, 34(7), 1337-1347; 2004.

[0075] 1-(p-Tolylsulfonyl)aziridine-2-carbaldehyde (C-3262) was prepared as described by Lapinsky, D. J. and Bergmeier, S. C. Tetrahedron Letters, 42(49), 8583-8586; 2001.

[0076] 1-Butylphenyl)sulfonylaziridine-2-carbaldehyde (C-3273) was prepared using the same method.

[0077] 1-(p-Tolylsulfonyl)aziridin-2-yl]ethanone (C-3263) was prepared as described by Smith, A. B., and Kim, D.-S. Journal of Organic Chemistry, 71(7), 2547-2557; 2006.

[0078] 1-(4-Butylphenyl)sulfonylaziridin-2-yl]ethanone (C-3272) was prepared using the same method.

[0079] Methyl (2S)-1-(p-tolylsulfonyl)aziridine-2-carboxylate (C-3535) was prepared as described by Qian, G.; Bai, M.; Gao, S.; Chen, H.; Zhou, S.; Cheng, H-G.; Yan, W.; Zhou, Q. Angewandte Chemie, International Edition (2018), 57(34), 10980-10984.

[0080] Methyl (2R)-1-(p-tolylsulfonyl)aziridine-2-carboxylate (C-3539) was prepared as described by Smith, A. B. and Kim, D-S. Journal of Organic Chemistry (2006), 71(7), 2547-2557.

[0081] Methyl (2S)-1-[[6-(dimethylamino)-1-naphthyl]sulfonyl]aziridine-2-carboxylate (C-3548) and methyl (2R)-1-[[6-(dimethylamino)-1-naphthyl]sulfonyl]aziridine-2-carboxylate (C-3570) were prepared using methodology as described by Smith, A. B. and Kim, D-S. Journal of Organic Chemistry (2006), 71(7), 2547-2557.

[0082] Lithium 1-tosylaziridine-2-carboxylate (C-3612) was prepared as described by Baldwin, J. E.; Spivey, A. C.; Schofield, C. J.; Sweeney, J. B. Tetrahedron, 49(28), 6309-30; 1993

[0083] Synthesis of 6-(dimethylamino)-5-formylnaphthalene-1-sulfonyl chloride.

##STR00025##

Into a 50 mL round-bottom flask, was placed 6-(dimethylamino)naphthalene-1-sulfonic acid (1.0 g, 3.98 mmol). To this was added CH.sub.2Cl.sub.2 (20 mL). To the mixture was added DMF (0.4 mL). To the above was added dropwise oxalyl dichloride (2.0 g, 15.74 mmol). The resulting solution was allowed to react with stirring for 24 h at room temperature. The reaction mixture was then quenched by the adding 50 mL of ice/salt. The resulting solution was extracted twice with 10 mL of CH.sub.2Cl.sub.2 and the organic layers combined and dried over Na.sub.2SO.sub.4. Solvent was evaporated under vacuum. The resulted 6-(dimethylamino)-5-formylnaphthalene-1-sulfonyl chloride (0.83 g 70%) was used on the next stage without additional purification. .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 10.30 (s, 1 H), 9.55 (dt, J=8.7, 1.0 Hz, 1 H), 8.87 (dd, J=9.7, 0.9 Hz, 1 H), 8.18 (dd, J=7.6, 1.1 Hz, 1 H), 7.66 (dd, J=8.7, 7.6 Hz, 1 H), 7.60 (d, J=9.7 Hz, 1 H), 3.22 (s, 6 H).

[0084] The same method was used for the preparation of 6-(dimethylamino)-5-formylnaphthalene-2-sulfonyl chloride.

##STR00026##

.sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 10.26 (s, 1 H), 8.91 (d, J=9.1 Hz, 1 H), 8.11 (d, J=9.1 Hz, 1 H), 8.11 (m, 1 H), 7.75 (dd, J=9.1, 2.0 Hz, 1 H), 7.51 (d, J=9.1 Hz, 1 H), 7.41 (d, J=9.1 Hz, 1 H), 3.13 (s, 6 H).

[0085] Synthesis of 5-chloro-6-(methylamino)naphthalene-2-sulfonyl chloride.

##STR00027##

To a suspension of 6-(dimethylamino)naphthalene-2-sulfonic acid (1.0 g, 3.98 mmol). in POCl.sub.3 (5 mL) was slowly added PCl.sub.5 (3.7 g, 17.8 mmol). The resulting mixture was heated at 50° C. for 5 h before it was allowed to cool to room temperature and poured onto crushed ice. The aqueous mixture was stirred vigorously at 0° C. for 40 min. Product was extracted twice with 40 mL of CH.sub.2Cl.sub.2 and the organic layers combined and dried over Na.sub.2SO.sub.4. Solvent was evaporated under vacuum. The resulted 5-chloro-6-(methylamino)naphthalene-2-sulfonyl chloride was purified by chromatography (silica gel, petroleum ether/ethyl acetate 4:1). Yield 0.35 g (30%). .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.24 (d, J=2.0 Hz, 1 H), 8.15 (dt, J=9.2, 0.6 Hz, 1 H), 7.95 (dd, J=9.2, 2.0 Hz, 1 H), 7.86 (d, J=9.0 Hz, 1 H), 7.22 (d, J=9.0 Hz, 1 H), 3.11 (s, 3 H).

TABLE-US-00001 Characteristics of aromatic sulfonamides C-3161 Methyl 1-(p-tolylsulfonyl)aziridine-2-carboxylate Molecular formula: C.sub.11H.sub.13NO.sub.4S; Molecular weight: 255.29; Melting point: 56-58° C.; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.84 (d, J=8.3 Hz, 2 H), 7.35 (d, J=8.3 Hz, 2 H), 3.74 (s, 3 H), 3.34 (dd, J=7.1, 4.1 Hz, 1 H), 2.76 (d, J=7.1 Hz, 1 H), 2.56 (d, J=4.1 Hz, 1 H), 2.45 (s, 3 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.2, 145.2, 134.0, 129.9, 128.2, 52.9, 35.7, 32.0, 21.7; LCMS ESI.sup.- (m/z): 254.2 [M-H].sup.-, LCMS purity 100.00% C-3212 Methyl 1-(4-nitrophenyl)sulfonylaziridine-2-carboxylate Molecular formula: C.sub.10H.sub.10N.sub.2O.sub.6S; Molecular weight: 286.26; Melting point: 106-108° C.; .sup.1H- NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.41 (d, J=9.0 Hz, 2 H), 8.18 (d, J=9.0 Hz,2 H), 3.76 (s, 3 H), 3.46 (dd, J=7.1, 4.3 Hz, 1 H), 2.89 (d, J=7.1 Hz, 1 H), 2.66 (d, J=4.3 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 166.6, 150.9, 142.9, 129.5, 124.5, 53.1, 35.2, 32.5; LCMS ESI.sup.- (m/z): 285.1 [M-H].sup.-, LCMS purity 100.00% C-3216 1-(4-Nitrophenyl)sulfonylaziridine-2-carboxamide Molecular formula: C.sub.9H.sub.9N.sub.3O.sub.5S; Molecular weight: 271.25; Melting point: 179-181° C.; .sup.1H- NMR spectrum (400 MHz): (DMSO-d6, HMDSO) δ: 8.47 (d, J=8.9 Hz, 2 H), 8.24 (d, J=8.8 Hz, 2 H), 7.87 (br s, 1 H), 7.47 (br s, 1 H), 3.39 (dd, J=7.2, 4.5 Hz, 1 H), 2.79 (d, J=7.2 Hz, 1 H), 2.58 (d, J=4.5 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (DMSO-d6, HMDSO) δ: 166.5, 151.2, 142.6, 130.0, 125.3, 37.6, 32.2; LCMS ESI.sup.+ (m/z): 271.9 [M+H].sup.+; Impurities: 3.67% (210 nm); 2.24% (254 nm) C-3218 1-(4-Aminophenyl)sulfonylaziridine-2-carboxamide Molecular formula: C.sub.9H.sub.11N.sub.3O.sub.3S; Molecular weight: 241.27; Melting point: 139-141° C.; .sup.1H- NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.72 (s, 1 H), 7.50 (d, J=8.7 Hz, 2 H), 7.34 (s, 1 H), 6.65 (d, J=8.7 Hz, 2 H), 6.25 (s, 2 H), 3.01 (dd, J=7.1, 4.1 Hz, 1 H), 2.41 (d, J=7.1 Hz, 1 H), 2.35 (d, J=4.1 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (DMSO-d.sub.6, HMDSO) δ: 167.5, 154.6, 130.5, 120.5, 113.2, 36.8, 31.2; LCMS ESI.sup.- (m/z): 242.2 [M-H].sup.-, LCMS purity 100.00% C-3220 1-(p-Tolylsulfonyl)aziridine-2-carboxamide Molecular formula: C.sub.10H.sub.12N.sub.2O.sub.3S; Molecular weight: 240.28; Melting point: 118-120° C.; .sup.1H- NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.82 (d, J=8.2 Hz, 2 H), 7.37 (d, J=8.2 Hz, 2 H), 6.11 (s, 1 H), 5.76 (s, 1 H), 3.23 (dd, J=7.7, 4.2 Hz, 1 H), 2.80 (d, J=7.7 Hz, 1 H), 2.48 (s, 3 H), 2.43 (d, J=4.2 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 168.3, 145.6, 133.4, 130.0, 128.2, 37.6, 33.1, 21.7; LCMS ESI.sup.- (m/z): 241.2 [M-H].sup.-, LCMS purity 100.00% C-3251 Methyl 1-(benzenesulfonyl)aziridine-2-carboxylate Molecular formula: C.sub.10H.sub.11NO.sub.4S; Molecular weight: 241.26; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3) δ: 7.00-8.94 (m, 2 H), 7.71-7.64 (m, 1 H), 7.60-7.53 (m, 2 H), 3.74 (s, 3 H), 3.37 (dd, J=7.1, 4.1 Hz, 1 H), 2.79 (d, J=7.1 Hz, 1 H), 2.58 (d, J=4.1 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3) δ: 167.3, 137.2, 134.3, 129.4, 128.3, 53.1, 35.9, 32.3; LCMS ESI.sup.+ (m/z): 242.1 [M+H].sup.+, LCMS purity 100.00% C-3256 Methyl 1-[4-(trifluoromethyl)phenyl]sulfonylaziridine-2-carboxylate Molecular formula: C.sub.11H.sub.10F.sub.3NO.sub.4S; Molecular weight: 309.26; Melting point: 68-70° C.; .sup.1H- NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.12 (d, J=8.4 Hz, 2 H), 7.84 (d, J=8.4 Hz, 2 H), 3.76 (s, 3 H), 3.43 (dd, J=7.1, 4.2 Hz, 1 H), 2.85 (dd, J=7.1, 0.9 Hz, 1 H), 2.63 (dd, J=4.2, 0.9 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 166.8, 140.8, 135.7 (q, J=33.1 Hz), 128.7, 126.4 (q, J=3.7 Hz), 123.0 (q, J=273.4 Hz), 53.0, 36.0, 32.3; LCMS ESI.sup.- (m/z): 308.2 [M-H].sup.-, LCMS purity 100.00% C-3257 Methyl 1-(4-butylphenyl)sulfonylaziridine-2-carboxylate Molecular formula: C.sub.14H.sub.19NO.sub.4 S; Molecular weight: 297.37; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.86 (d, J=8.4 Hz, 2 H), 7.36 (d, J=8.4 Hz, 2 H), 3.74 (s, 3 H), 3.35 (dd, J=7.1, 4.1 Hz, 1 H), 2.76 (d, J=7.1 Hz, 1 H), 2.70 (t, J=7.7 Hz, 2 H), 2.56 (d, J=4.1 Hz, 1 H), 1.58-1.67 (m, 2 H), 1.36 (sextet, J=7.5 Hz, 2 H), 0.94 (d, J=7.4 Hz, 3 H); .sup.13C- NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.3, 150.1, 134.1, 129.2, 128.2, 52.9, 35.6, 35.6, 32.1, 32.1, 22.2, 13.8; LCMS ESI.sup.+ (m/z): 298.2 [M+H].sup.+, LCMS purity 100% C-3262 1 -(p-Tolylsulfonyl)aziridine-2-carbaldehyde Molecular formula: C.sub.10H.sub.11NO.sub.4S; Molecular weight: 225.26; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.95 (d, J=5.9 Hz, 1 H), 7.84 (d, J=8.3 Hz, 2 H), 7.38 (d, J=8.3 Hz, 2 H), 3.27 (ddd, J=7.4, 5.9, 4.0 Hz, 1 H), 2.93 (d, J=7.4 Hz, 1 H), 2.58 (d, J=4.0 Hz, 1 H), 2.47 (s, 3 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 194.3, 145.6, 133.7, 130.0, 128.2, 41.9, 30.1, 21.7; LCMS ESI.sup.+ (m/z): 226.2 [M+H].sup.+, LCMS purity 94.70% C-3263 1-[1-(p-Tolylsulfonyl)aziridin-2-yl]ethanone Molecular formula: C.sub.11H.sub.13NO.sub.3S; Molecular weight: 239.29; Melting point: 90-92° C.; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.84 (d, J=8.3 Hz, 2 H), 7.37 (d, J=8.3 Hz, 2 H), 3.29 (dd, J=7.4, 4.1 Hz, 1 H), 2.80 (d, J=7.1 Hz, 1 H), 2.49 (d, J=4.1 Hz, 1 H), 2.46 (s, 3 H), 2.07 (s, 3H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 201.4, 145.3, 133.9, 129.9, 128.1, 41.9, 31.8, 25.9, 21.7; LCMS ESI.sup.+ (m/z): 240.2 [M+H]+ , LCMS purity 100%; Elemental analysis: Found [%]: C 55.07, H 5.35, N 5.74; Calculated [%]: C 55.21, H 5.48, N 5.85 C-3270 Methyl 1-(4-dodecylphenyl)sulfonylaziridine-2-carboxylate Molecular formula: C.sub.22H.sub.35NO.sub.4S; Molecular weight: 409.58; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.86 (d, J=8.4 Hz, 2 H), 7.35 (d, J=8.4 Hz, 2 H), 3.74 (s, 3 H), 3.36 (dd, J=7.1, 4.1 Hz, 1 H), 2.77 (d, J=7.1 Hz, 1 H), 2.69 (t, J=7.7 Hz, 2 H), 2.56 (d, J=4.1 Hz, 1 H), 1.63 (quintet, J=7.5 Hz, 2 H), 1.20-1.38 (m, 18 H), 0.87 (d, J=6.9 Hz, 3 H); .sup.13C- NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.3, 150.2, 134.1, 129.2, 128.2, 52.9, 36.0, 35.6, 32.1, 31.9, 29.6, 29.5, 29.4, 29.3, 29.2, 22.7, 14.1; LCMS ESI.sup.+ (m/z): 410.4 [M+H].sup.+, LCMS purity 100.00% C-3271 Methyl 1-(4-butoxyphenyl)sulfonylaziridine-2-carboxylate Molecular formula: C.sub.14H.sub.19NO.sub.5S; Molecular weight: 313.37; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.87 (d, J=8.4 Hz, 2 H), 7.00 (d, J=8.4 Hz, 2 H), 4.04 (t, J=6.5 Hz, 2 H), 3.74 (s, 3 H), 3.32 (dd, J=7.1, 4.1 Hz, 1 H), 2.74 (d, J=7.1 Hz, 1 H), 2.55 (d, J=4.1 Hz, 1 H), 1.80 (quintet, J=6.7 Hz, 2 H), 1.50 (sextet, J=7.5 Hz, 2 H), 0.99 (t, J=7.4 Hz, 3 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.3, 163.7, 130.4, 127.9, 114.9, 68.3, 52.8, 35.6, 32.0, 30.9, 19.1, 13.7; LCMS ESI.sup.+ (m/z): 314.3 [M+H].sup.+; LCMS purity 93.03% C-3272 1-[1-(4-Butylphenyl)sulfonylaziridin-2-yl] ethanone Molecular formula: C.sub.14H.sub.19NO.sub.3S; Molecular weight: 281.37; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.84 (d, J=8.4 Hz, 2 H), 7.36 (d, J=8.3 Hz, 2 H), 3.29 (dd, J=7.4, 4.1 Hz, 1 H), 2.70 (t, J=7.7 Hz, 2 H), 2.79 (d, J=7.4 Hz, 1 H), 2.49 (d, J=4.1 Hz, 1 H), 2.46 (s, 3 H), 2.07 (s, 3 H), 1.57-1.67 (m, 2 H), 1.36 (sextet, J=7.5 Hz, 2 H), 0.93 (t, J=7.4 Hz, 3 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 201.5, 150.2, 134.0, 129.3, 128.2, 41.9, 35.6, 33.0, 31.9, 25.9, 22.2, 13.8; LCMS ESI.sup.+ (m/z): 282.3 [M+H].sup.+, LCMS purity 96.65% C-3273 1-(4-Butylphenyl)sulfonylaziridine-2-carbaldehyde Molecular formula: C.sub.13H.sub.17NO.sub.3S; Molecular weight: 267.34; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.96 (d, J=5.8 Hz, 1 H), 7.85 (d, J=8.4 Hz, 2 H), 7.38 (d, J=8.3 Hz, 2 H), 3.28 (ddd, J=7.4, 5.8, 4.0 Hz, 1 H), 2.93 (d, J=7.4 Hz, 1 H), 2.71 (t, J=7.8 Hz, 2 H), 2.58 (d, J=4.0 Hz, 1 H), 1.57-1.68 (m, 2 H), 1.37 (sextet, J=7.5 Hz, 2 H), 0.94 (t, J=7.5 Hz, 3 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 194.3, 150.4, 133.8, 129.4, 128.2, 41.8, 35.6, 33.0, 30.1, 22.2, 13.8; LCMS ESI.sup.+ (m/z): 268.4 [M+H].sup.+, LCMS purity 100.00% C-3281 Methyl 1-(4-pentylphenyl)sulfonylaziridine-2-carboxylate Molecular formula: C.sub.15H.sub.21NO.sub.4S; Molecular weight: 311.40; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: (CDCl.sub.3, HMDSO) δ: 7.86 (d, J=8.4 Hz, 2 H), 7.39 (d, J=8.4 Hz, 2 H), 3.74 (s, 3 H), 3.36 (dd, J=7.1, 4.1 Hz, 1 H), 2.77 (d, J=7.1 Hz, 1 H), 2.69 (t, J=7.8 Hz, 2 H), 2.56 (d, J=4.1 Hz, 1 H), 1.64 (quintet, J=7.5 Hz, 2 H), 1.27-1.40 (m, 4 H), 0.90 (t, J=7.0 Hz, 3 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.2, 150.1, 134.1, 129.2, 128.2, 52.8, 35.8, 35.6, 32.1, 31.3, 30.6, 22.4, 13.9; LCMS ESI.sup.+ (m/z): 312.4 [M+H].sup.+, LCMS purity 100.00% C-3287 Methyl 1-(4-hexylphenyl)sulfonylaziridine-2-carboxylate Molecular formula: C.sub.16H.sub.23NO.sub.4S; Molecular weight: 325.42; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3) δ: 7.88-7.83 (m, 2 H), 7.38-7.32 (m, 2 H), 3.74 (s, 3 H), 3.35 (dd, J=7.1, 4.1 Hz, 1 H), 2.76 (d, J=7.1 Hz, 1 H), 2.73-2.65 (m, 2 H), 2.56 (d, J=4.1 Hz, 1 H), 1.68-1.58 (m, 2 H), 1.38-1.24 (m, 6 H), 0.92-0.84 (m, 3 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3) δ: 167.4, 150.3, 134.3, 129.4, 128.4, 53.0, 36.1, 35.8, 32.2, 31.7, 31.1, 29.0, 22.7, 14.2; LCMS ESI+ (m/z): 326.2 [M+H]+ , LCMS purity 99.43% C-3288 Methyl 1-(4-heptylphenyl)sulfonylaziridine-2-carboxylate Molecular formula: C.sub.17H.sub.25NO.sub.4S; Molecular weight: 339.45; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.86 (d, J=8.5 Hz, 2 H), 7.36 (d, J=8.5 Hz, 2 H), 3.74 (s, 3 H), 3.36 (dd, J=7.1, 4.1 Hz, 1 H), 2.77 (d, J=7.1 Hz, 1 H), 2.69 (t, J=7.7 Hz, 2 H), 2.56 (d, J=4.1 Hz, 1 H), 1.63 (quintet, J=7.5 Hz, 2 H), 1.22-1.37 (m, 8 H), 0.88 (t, J=7.1 Hz, 3 H); .sup.13C- NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.3, 150.1, 134.1, 129.2, 128.2, 52.9, 35.9, 35.6, 32.1, 31.7, 31.0, 29.1, 29.0, 22.6, 14.0; LCMS ESI.sup.+ (m/z): 340.4 [M+H].sup.+, LCMS purity 100.00% C-3290 Methyl 1-(4-tert-butylphenyl)sulfonylaziridine-2-carboxylate Molecular formula: C.sub.14H.sub.19NO.sub.4S; Molecular weight: 297.37; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.88 (d, J=8.6 Hz, 2 H), 7.57 (d, J=8.6 Hz, 2 H), 3.74 (s, 3 H), 3.37 (dd, J=7.1, 4.1 Hz, 1 H), 2.76 (d, J=7.1 Hz, 1 H), 2.56 (d, J=4.1 Hz, 1 H), 1.35 (s, 9 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.3, 158.1, 133.9, 128.0, 126.3, 52.9, 35.6, 35.3, 32.1, 31.0; LCMS ESI.sup.+ (m/z): 398.3 [M+H].sup.+, LCMS purity 100.00% C-3291 Methyl 1-(4-phenylphenyl)sulfonylaziridine-2-carboxylate Molecular formula: C.sub.16H.sub.15NO.sub.4S; Molecular weight: 317.36; Melting point: 90-92° C.; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.03 (d, J=8.8 Hz, 2 H), 7.77 (d, J=8.8 Hz, 2 H), 7.60-7.62 (m, 2 H), 7.41-7.52 (m, 3 H), 3.76 (s, 3 H), 3.41 (dd, J=7.1, 4.1 Hz, 1 H), 2.82 (d, J=7.1 Hz, 1 H), 2.61 (d, J=4.1 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.2, 147.1, 139.0, 135.5, 129.1, 128.7, 128.7, 127.9, 127.4, 52.9, 35.7, 32.1; LCMS ESI.sup.+ (m/z): 318.3 [M+H].sup.+, LCMS purity 100.00% C-3292 Methyl 1-(2-naphthylsulfonyl)aziridine-2-carboxylate Molecular formula: C.sub.14H.sub.13NO.sub.4S; Molecular weight: 291.32; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.52-8.54 (m, 1 H), 7.99-8.03 (m, 2 H), 7.93-7.97 (m, 2 H), 7.67-7.72 (m, 1 H), 7.62-7.67 (m, 1 H), 3.73 (s, 3 H), 3.44 (dd, J=7.1, 4.1 Hz, 1 H), 2.85 (d, J=7.1 Hz, 1 H), 2.60 (d, J=4.1 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.1, 135.5, 133.9, 132.0, 129.9, 129.6, 129.5, 129.5, 128.0, 127.8, 122.8, 52.9, 35.8, 32.1; LCMS ESI+ (m/z): 292.3 [M+H]+ , LCMS purity 97.48% C-3294 Methyl 1-(4-methoxyphenyl)sulfonylaziridine-2-carboxylate Molecular formula: C.sub.11H.sub.13NO.sub.5S; Molecular weight: 271.29; Melting point: 73-75° C.; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.89 (d, J=9.1 Hz, 2 H), 7.01 (d, J=9.1 Hz, 2 H), 3.89 (s, 3 H), 3.74 (s, 3 H), 3.32 (dd, J=7.1, 4.1 Hz, 1 H), 2.75 (d, J=7.1 Hz, 1 H), 2.55 (d, J=4.1 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.3, 164.1, 130.4, 128.3, 114.5, 55.7, 52.8, 35.7, 32.0; LCMS ESI+ (m/z): 272.3 [M+H]+ , LCMS purity 100% C-3295 Methyl 1-(4-isopropylphenyl)sulfonylaziridine-2-carboxylate Molecular formula: C.sub.13H.sub.17NO.sub.4S; Molecular weight: 283.34; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.88 (d, J=8.6 Hz, 2 H), 7.40 (d, J=8.6 Hz, 2 H), 3.75 (s, 3 H), 3.36 (dd, J=7.1, 4.1 Hz, 1 H), 3.00 (septet, J=6.9 Hz, 1 H), 2.76 (d, J=7.1 Hz, 1 H), 2.56 (d, J=4.1 Hz, 1 H), 1.28 (d, J=6.9 Hz, 6 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.3, 155.9, 134.2, 128.3, 127.4, 52.8, 35.6, 34.2, 32.1, 23.5; LCMS ESI+ (m/z): 284.3 [M+H]+ , LCMS purity 100% C-3296 Methyl 1-(4-chlorophenyl)sulfonylaziridine-2-carboxylate Molecular formula: C.sub.10H.sub.10ClNO.sub.4S; Molecular weight: 275.71; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.91 (d, J=8.7 Hz, 2 H), 7.55 (d, J=8.7 Hz, 2 H), 3.75 (s, 3 H), 3.38 (dd, J=7.1, 4.1 Hz, 1 H), 2.80 (d, J=7.1 Hz, 1 H), 2.60 (d, J=4.1 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 166.9, 140.9, 135.6, 129.6, 129.6, 53.0, 35.9, 32.2; LCMS ESI.sup.+ (m/z): 276.2 [M+H].sup.+, LCMS purity 100.00% C-3297 Methyl 1-(2-fluoro-4-methyl-phenyl)sulfonylaziridine-2-carboxylate Molecular formula: C.sub.11H.sub.12FNO.sub.4S; Molecular weight: 273.26; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.82 (dd, J=8.0, 7.3 Hz, 1 H), 7.10-7.13 (m, 1 H), 7.04-7.08 (m, 1 H), 3.77 (s, 3 H), 3.50 (ddd, J=7.1, 4.3, 0.9 Hz, 1 H), 2.95 (dd, J=7.1, 1.2 Hz, 1 H), 2.66 (d, J=4.3 Hz, 1 H), 2.44 (s, 3 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.2, 159.3 (d, J=258.3 Hz,), 148.8 (d, J=8.5 Hz,), 130.3, 125.2 (d, J=3.0 Hz,), 122.4 (d, J=14.5 Hz,), 117.8 (d, J=20.9 Hz,),, 52.9, 35.9, 32.4, 21.6; LCMS ESI.sup.+ (m/z): 274.3 [M+H].sup.+, LCMS purity 96.13% C-3299 Methyl 1-(4-propylphenyl)sulfonylaziridine-2-carboxylate Molecular formula: C.sub.13H.sub.17NO.sub.4S; Molecular weight: 283.34; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.86 (d, J=8.5 Hz, 2 H), 7.36 (d, J=8.5 Hz, 2 H), 3.74 (s, 3 H), 3.36 (dd, J=7.1, 4.1 Hz, 1 H), 2.77 (d, J=7.1 Hz, 1 H), 2.68 (t, J=7.6 Hz, 2 H), 2.56 (d, J=4.1 Hz, 1 H), 1.68 (sextet, J=7.5 Hz, 2 H), 0.95 (t, J=7.4 Hz, 3 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: (CDCl.sub.3, HMDSO) δ: 167.2, 149.8, 134.2, 129.3, 128.2, 52.9, 37.9, 35.6, 32.1, 24.1, 13.6; LCMS ESI.sup.+ (m/z): 284.3 [M+H].sup.+, LCMS purity 100.00% C-3303 Methyl 1-(m-tolylsulfonyl)aziridine-2-carboxylate Molecular formula: C.sub.11H.sub.13NO.sub.4S; Molecular weight: 255.29; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.88-7.80 (m, 1 H), 7.74-7.77 (m, 1 H), 7.46-7.50 (m, 1 H), 7.42-7.46 (m, 1 H), 3.74 (s, 3 H), 3.37 (dd, J=7.1, 4.1 Hz, 1 H), 2.78 (d, J=7.1 Hz, 1 H), 2.57 (d, J=4.1 Hz, 1 H), 2.45 (s, 3 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.2, 139.6, 136.8, 135.0, 129.1, 128.5, 125.2, 52.9, 35.6, 32.1, 24.3; LCMS ESI.sup.+ (m/z): 256.2 [M+H].sup.+, LCMS purity 97.26% C-3304 Methyl 1-(4-propylphenyl)sulfonylaziridine-2-carboxylate Molecular formula: C.sub.13H.sub.17NO.sub.4S; Molecular weight: 283.34; Melting point:106-108° C. .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 6.98 (s, 2 H), 3.74 (s, 3 H), 3.34 (dd, J=7.1, 4.1 Hz, 1 H), 2.79 (d, J=7.1 Hz, 1 H), 2.69 (s, 6 H), 2.51 (d, J=4.1 Hz, 1 H), 2.32 (s, 3 H); .sup.13C- NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.5, 143.6, 140.4, 131.9, 131.7, 52.7, 34.7, 31.7, 22.9, 21.0 LCMS ESI+ (m/z): 284.3 [M+H]+ , LCMS purity 100% C-3305 Methyl 1-[3-(trifluoromethyl)phenyl]sulfonylaziridine-2-carboxylate Molecular formula: C.sub.11H.sub.10F.sub.3NO.sub.4S; Molecular weight: 309.26; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.23-8.26 (m, 1 H), 8.16-8.20 (m, 1 H), 7.92-7.96 (m, 1 H), 7.71-7.77 (m, 1 H), 3.76 (s, 3 H), 3.45 (dd, J=7.1, 4.2 Hz, 1 H), 2.86 (dd, J=7.1, 0.9 Hz, 1 H), 2.64 (dd, J=4.2, 0.9 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 166.8, 138.5, 132.0 (q, J=34.1 Hz), 131.4, 130.8 (q, J=3.6 Hz), 130.1, 125.2 (q, J=3.8 Hz), 123.0 (q, J=273.8 Hz), 53.0, 36.0, 32.4; LCMS ESI- (m/z): 310.2 [M+H].sup.+, LCMS purity 100.00% C-3308 Methyl 1-(4-acetamidophenyl)sulfonylaziridine-2-carboaylate Molecular formula: C.sub.12H.sub.14N.sub.2O.sub.5S; Molecular weight: 298.31; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: (CDCl.sub.3, HMDSO) δ: 7.73-7.95 (m, 3 H), 7.67 (d, J=8.9 Hz, 2 H), 3.74 (s, 3 H), 3.43 (dd, J=7.1, 4.1 Hz, 1 H), 2.76 (d, J=7.1 Hz, 1 H), 2.56 (d, J=4.1 Hz, 1 H), 2.21 (s, 3 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 168.9, 167.4, 143.4, 131.0, 129.5, 119.3, 53.0, 35.7, 32.1, 24.7; LCMS ESI.sup.+ (m/z): 299.2 [M+H].sup.+, LCMS purity 94.91% C-3311 Methyl 1-(1-naphthylsulfonyl)aziridine-2-carboxylate Molecular formula: C.sub.14H.sub.13NO.sub.4S; Molecular weight: 291.32; Melting point: 102-104° C.; .sup.1H- NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.90 (ddd, J=8.6, 1.8, 0.8 Hz, 1 H), 8.24 (dd, J=7.4, 1.3 Hz, 1 H), 8.15 (dt, J=8.2, 1.2 Hz, 1 H), 7.95 (ddd, J=8.2, 1.3, 0.6 Hz, 1 H), 7.73 (ddd, J=8.2, 6.9, 1.3 Hz, 1 H), 7.63 (ddd, J=8.2, 6.9, 1.2 Hz, 1 H), 7.57 (dd, J=8.2, 7.4 Hz, 1 H), 3.70 (s, 3 H), 3.49 (dd, J=7.1, 4.1 Hz, 1 H), 2.89 (d, J=7.1 Hz, 1 H), 2.59 (d, J=4.1 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.1, 135.7, 134.2, 132.6, 130.0, 129.0, 128.7,128.6, 127.2, 125.5, 124.0, 52.8, 35.9, 32.5; LCMS ESI+ (m/z): 292.3 [M+H]+, LCMS purity 98.48% C-3314 1-(p-Tolylsulfonyl)aziridine-2-carbonitrile Molecular formula: C.sub.10H.sub.10N.sub.2O.sub.2S; Molecular weight: 222.26; Melting point: 83-85° C.; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.85 (d, J=8.4 Hz, 2 H), 7.41 (d, J=8.4 Hz, 2 H), 3.22 (dd, J=7.0, 4.0 Hz, 1 H), 2.89 (d, J=7.0 Hz, 1 H), 2.65 (d, J=4.0 Hz, 1 H), 2.49 (s, 3 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 146.1, 133.1, 130.2, 128.2, 115.0, 32.1, 23.4, 21.7; LCMS ESI- (m/z): 221.2 [M-H]-, LCMS purity 100.00% C-3316 Methyl 1-(4-cyclohexylphenyl)sulfonylaziridine-2-carboxylate Molecular formula: C.sub.16H.sub.21NO.sub.4S; Molecular weight: 323.12; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.87 (d, J=8.5 Hz, 2 H), 7.38 (d, J=8.5 Hz, 2 H), 3.74 (s, 3 H), 3.36 (dd, J=7.1, 4.1 Hz, 1 H), 2.76 (d, J=7.1 Hz, 1 H), 2.56-2.65 (m, 1 H), 2.56 (d, J=4.1 Hz, 1 H), 1.82-1.94 (m, 4 H), 1.73-1.82 (m, 1 H), 1.34-1.50 (m, 4 H), 1.20-1.33 (m, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.3, 155.0, 134.1, 128.3, 127.7, 52.8, 44.6, 35.5, 34.0, 32.1, 26.6, 25.9; LCMS ESI.sup.+ (m/z): 324.3 [M+H].sup.+, LCMS purity 98.89% C-3319 Methyl 1-(4-octylphenyl)sulfonylaziridine-2-carboxylate Molecular formula: C.sub.18H.sub.27NO.sub.4S; Molecular weight: 353.48; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.86 (d, J=8.5 Hz, 2 H), 7.36 (d, J=8.5 Hz, 2 H), 3.74 (s, 3 H), 3.36 (dd, J=7.1, 4.1 Hz, 1 H), 2.77 (d, J=7.1 Hz, 1 H), 2.69 (t, J=7.7 Hz, 2 H), 2.56 (d, J=4.1 Hz, 1 H), 1.63 (quintet, J=7.6 Hz, 2 H), 1.22-1.36 (m, 10 H), 0.88 (t, J=7.1 Hz, 3 H); .sup.13C- NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.3, 150.1, 134.1, 129.2, 128.2, 52.8, 35.9, 35.6, 32.1, 31.8, 31.0, 29.3, 29.1, 29.0, 22.6, 14.0; LCMS ESI.sup.+ (m/z): 354.4 [M+H].sup.+, LCMS purity 100.00% C-3320 Methyl 1-(o-tolylsulfonyl)aziridine-2-carboxylate Molecular formula: C.sub.11H.sub.13NO.sub.4S; Molecular weight: 255.29; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.94 (dd, J=7.8, 1.4 Hz, 1 H), 7.53 (dt, J=7.5, 1.4 Hz, 1 H), 7.32-7.39 (m, 2 H), 3.75 (s, 3 H), 3.38 (dd, J=7.1, 4.1 Hz, 1 H), 2.83 (d, J=7.1 Hz, 1 H), 2.79 (s, 3 H), 2.55 (d, J=4.1 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.3, 139.4, 135.6, 134.0, 132.7, 129.5, 126.1, 52.8, 35.4, 32.2, 20.6; LCMS ESI.sup.+ (m/z): 256.2 [M+H].sup.+, LCMS purity 100.00% C-3324 1-[4-(Trifluoromethyl)phenyl] sulfonylaziridine-2-carboxamide Molecular formula: C.sub.10H.sub.9F.sub.3N.sub.2O.sub.3S; Molecular weight: 294.25; Melting point: 138-140° C.; .sup.1H- NMR spectrum (400 MHz): (DMSO-d.sub.6, HMDSO) δ: 8.19 (d, J=8.3 Hz, 2 H), 8.08 (d, J=8.3 Hz, 2 H), 7.86 (br s, 1 H), 7.45 (br s, 1 H), 3.36 (dd, J=7.2, 4.5 Hz, 1 H), 2.76 (d, J=7.2, 1 H), 2.56 (d, J=4.5, 1 H); .sup.13C-NMR spectrum (100 MHz): (DMSO-d.sub.6, HMDSO) δ: 166.6, 141.2, 133.9 (q, J=32.7 Hz), 129.2, 127.3 (q, J=3.6 Hz), 123.6 (q, J=273.4 Hz), 37.5, 32.0; LCMS ESI.sup.+ (m/z): 295.2 [M+H].sup.+, LCMS purity 100.00% C-3326 Methyl 1-[[5-(dimethylamino)-1-naphthyl]sulfonyl]aziridine-2-carboaylate Molecular formula: C.sub.16H.sub.18N.sub.2O.sub.4S; Molecular weight: 334.39; Melting point: 117-119° C.; .sup.1H- NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.63 (dt, J=8.5, 1.1 Hz, 1 H), 8.55 (dt, J=8.7, 0.9 Hz, 1 H), 8.22 (dd, J=7.4, 1.3 Hz, 1 H), 7.61 (dd, J=8.7, 7.6 Hz, 1 H), 7.54 (dd, J=8.5, 7.4 Hz, 1 H), 7.21 (dd, J=7.6, 0.9 Hz, 1 H), 3.74 (s, 3 H), 3.49 (dd, J=7.1, 4.2 Hz, 1 H),), 2.89 (s, 6 H), 2.87 (d, J=7.1 Hz, 1 H), 2.58 (d, J=4.2 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.2, 151.7, 132.7, 131.9, 130.4, 129.9, 129.9, 128.7, 123.0, 120.0, 115.5, 52.8, 45.4, 35.8, 32.5; LCMS ESI.sup.+ (m/z): 335.1 [M+H].sup.+, LCMS purity 100.00% C-3327 Methyl 1-[(6-methoxy-2-naphthyl)sulfonyl]aziridine-2-carboxylate Molecular formula: C.sub.15H.sub.15NO.sub.5S; Molecular weight: 321.35; Melting point: 97-99° C.; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.42-8.44 (m, 1 H), 7.85-7.93 (m, 3 H), 7.28 (dd, J=9.0, 2.5 Hz, 1 H), 7.20 (d, J=2.5 Hz, 1 H), 3.97 (s, 3 H), 3.73 (s, 3 H), 3.41 (dd, J=7.1, 4.1 Hz, 1 H), 2.82 (d, J=7.1 Hz, 1 H), 2.58 (d, J=4.1 Hz, 1 H); .sup.13 C-NMR spectrum (100 MHz): (CDCl.sub.3,HMDSO) δ: 167.2, 160.4, 137.4, 131.3, 131.0, 129.8, 128.1, 127.3, 123.6, 120.9, 105.9, 55.5, 52.9, 35.7, 32.1; LCMS ESI.sup.+ (m/z): 322.2 [M+H].sup.+, LCMS purity 95.29% C-3329 Methyl 1-[(6-methyl-2-naphthyl)sulfonyl]aziridine-2-carboxylate Molecular formula: C.sub.15H.sub.15NO.sub.4S; Molecular weight: 305.07; Melting point: 91-93° C.; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.63-8.66 (m, 1 H), 8.21 (dd, J=7.4, 1.3 Hz, 1 H), 8.9 (dt, J=8.2, 1.2 Hz, 1 H), 7.84 (d, J=1.4 Hz, 1 H), 7.48 (dd, J=8.2, 7.4 Hz, 1 H), 7.46 (dd, J=8.4, 1.6 Hz, 1 H), 3.71 (s, 3 H), 3.50 (dd, J=7.1, 4.1 Hz, 1 H), 2.88 (d, J=7.1 Hz, 1 H), 2.61 (s, 3 H), 2.59 (d, J=4.1 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.2, 138.9, 135.4, 132.5, 131.7, 130.0, 129.4, 129.2, 128.5, 124.4, 123.0, 52.8, 35.9, 32.5, 22.4; LCMS ESI.sup.+ (m/z): 306.3 [M+H].sup.+, LCMS purity 98.42% C-3332 Methyl 1-(4-ethylphenyl)sulfonylaziridine-2-carboxylate Molecular formula: C.sub.12H.sub.15NO.sub.4S; Molecular weight: 269.07; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.87 (d, J=8.4 Hz, 2 H), 7.38 (d, J=8.4 Hz, 2 H), 3.74 (s, 3 H), 3.35 (dd, J=7.1, 4.1 Hz, 1 H), 2.71-2.78 (m, 3 H), 2.56 (d, J=4.1 Hz, 1 H), 1.27 (t, J=7.6 Hz, 3 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.2, 151.3, 134.1, 128.7, 128.3, 52.9, 35.6, 32.0, 28.9, 15.0; LCMS ESI.sup.+ (m/z): 270.3 [M+H].sup.+, LCMS purity 97.57% C-3336 Methyl 1-[(4-methyl-1-naphthyl)sulfonyl]aziridine-2-carboxylate Molecular formula: C.sub.15H.sub.15NO.sub.4S; Molecular weight: 305.07; Melting point: 96-98° C.; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.93 (d, J=8.8 Hz, 1 H), 8.13 (d, J=7.6 Hz, 1 H), 8.11 (dd, J=8.0, 1.1 Hz, 1 H), 7.72 (ddd, J=8.3, 6.9 Hz, 1.4 Hz, 1 H), 7.66 (ddd, J=8.3, 6.9 Hz, 1.4 Hz, 1 H), 7.41 (dd, J=7.6, 0.9 Hz, 1 H), 3.70 (s, 3 H), 3.46 (dd, J=7.1, 4.1 Hz, 1 H), 2.86 (d, J=7.1 Hz, 1 H), 2.79 (s, 3 H), 2.57 (d, J=4.1 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.2, 143.2, 133.3, 130.7, 129.8, 129.0, 128.2, 127.0, 126.1, 124.8, 124.7, 52.8, 35.8, 32.4, 20.2; LCMS ESI.sup.+ (m/z): 306.3 [M+H].sup.+, LCMS purity 100.00% C-3342 N,N-Dimethyl-1-(p-tolylsulfonyl)aziridine-2-carboxamide Molecular formula: C.sub.12H.sub.16N.sub.2O.sub.3S; Molecular weight: 268.33; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.85 (d, J=8.4 Hz, 2 H), 7.35 (d, J=8.4 Hz, 2 H), 3.59 (dd, J=6.9, 4.2 Hz, 1 H), 3.22 (s, 3 H), 2.97 (s, 3 H), 2.68 (d, J=4.2 Hz, 1 H), 2.64 (d, J=6.9 Hz, 1 H), 2.45 (s, 3 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 164.9, 145.1, 134.2, 129.8, 128.1, 37.2, 36.0, 35.2, 32.4, 21.6; LCMS ESI.sup.+ (m/z): 269.2 [M+H].sup.+, LCMS purity 100.00% C-3343 Methyl 1-[4-(dimethylamino)phenyl]sulfonylaziridine-2-carboxylate Molecular formula: C.sub.12H.sub.16N.sub.2O.sub.4S; Molecular weight: 284.33; Melting point: 84-86° C.; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.74 (d, J=9.1 Hz, 2 H), 6.68 (d, J=9.1 Hz, 2 H), 3.73 (s, 3 H), 3.25 (dd, J=7.1, 4.1 Hz, 1 H), 3.07 (s, 6 H), 2.67 (d, J=7.1 Hz, 1 H), 2.50 (d, J=4.1 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.6, 153.7, 130.1, 121.1, 110.9, 52.7, 40.0, 35.5, 31.8; LCMS ESI.sup.+ (m/z): 285.2 [M+H].sup.+, LCMS purity 100.00% C-3346 Methyl 1-(2-furylsulfonyl)aziridine-2-carboxylate Molecular formula: C.sub.8H.sub.9NO.sub.5S; Molecular weight: 231.02; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.67 (dd, J=1.8, 1.0 Hz, 1 H), 7.23 (dd, J=3.5, 1.0 Hz, 1 H), 6.58 (dd, J=3.5, 1.8 Hz, 1 H), 3.78 (s, 3 H), 3.42 (dd, J=7.1, 4.2 Hz, 1 H), 2.85 (d, J=7.1 Hz, 1 H), 2.68 (d, J=4.2 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 166.8, 147.9, 145.5, 111.6, 53.0, 35.9, 32.3; LCMS ESI.sup.+ (m/z): 232.1 [M+H].sup.+, LCMS purity 99.01% C-3350 Methyl 1-[(2-oxo-1H-quinolin-6-yl)sulfonyl]aziridine-2-carboxylate Molecular formula: C.sub.13H.sub.12N.sub.5O.sub.5S; Molecular weight: 308.31; Melting point: 139-141° C.; .sup.1H- NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 12.78 (br s, 1 H), 8.24 (d, J=2.0 Hz, 1 H), 8.05 (dd, J=8.7, 2.0 Hz, 1 H), 7.90 (d, J=9.6 Hz, 1 H), 7.67 (d, J=8.7 Hz, 1 H), 6.84 (d, J=9.6 Hz, 1 H), 3.74 (s, 3 H), 3.41 (dd, J=7.1, 4.1 Hz, 1 H), 2.84 (d, J=7.1 Hz, 1 H), 2.61 (d, J=4.1 Hz, 1 H); .sup.13C- NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.0, 164.6, 142.0, 140.7, 131.1, 129.4,129.1, 123.4, 119.4, 117.1, 53.0, 35.9, 32.2; LCMS ESI.sup.+ (m/z): 309.1 [M+H].sup.+, LCMS purity 96.88% C-3353 Methyl 1-(2,4-difluorophenyl)sulfonylaziridine-2-carboxylate Molecular formula: C.sub.10H.sub.9F.sub.2NO.sub.4S; Molecular weight: 277.24; Melting point: 40-42° C.; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.99 (ddd, J=7.9, 7.9, 7.9 Hz, 1 H), 7.03-7.08 (m, 1 H), 6.97-7.03 (m, 1 H), 3.77 (s, 3 H), 3.52 (ddd, J=7.2, 4.3, 0.9 Hz, 1 H), 2.97 (dd, J=7.2, 1.2 Hz, 1 H), 2.69 (d, J=4.3 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 166.9, 166.7 (dd, J=260.0, 11.6 Hz,), 160.5 (dd, J=261.0, 12.9 Hz,), 132.4 (d, J=10.8 Hz,), 122.1 (dd, J=14.5, 3.4 Hz,), 112.2 (dd, J=22.3, 3.5 Hz,), 106.0 (t, J=25.5 Hz,), 53.0, 36.1, 32.6; LCMS ESI.sup.+ (m/z): 276.3 [M+H].sup.+, LCMS purity 98.27% C-3355 Methyl 1-(2-oxochromen-6-yl)sulfonylaziridine-2-carboxylate Molecular formula: C.sub.13H.sub.11NO.sub.6S; Molecular weight: 309.29; Melting point: 42-44° C.; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 12.78 (br s, 1 H), 8.24 (d, J=2.0 Hz, 1 H), 8.05 (dd, J=8.7, 2.0 Hz, 1 H), 7.90 (d, J=9.6 Hz, 1 H), 7.67 (d, J=8.7 Hz, 1 H), 6.84 (d, J=9.6 Hz, 1 H), 3.74 (s, 3 H), 3.41 (dd, J=7.1, 4.1 Hz, 1 H), 2.84 (d, J=7.1 Hz, 1 H), 2.61 (d, J=4.1 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 166.8, 159.0, 157.3, 142.1, 133.4, 131.0, 128.7, 119.1, 118.7, 118.2, 53.0, 36.0, 32.3; LCMS ESI.sup.+ (m/z): 310.1 [M+H].sup.+, LCMS purity 100.00% C-3357 1-[4-(Dimethylamino)phenyl] sulfonyl-N,N-dimethyl-aziridine-2-carboxamide Molecular formula: C.sub.13H.sub.19N.sub.3O.sub.3S; Molecular weight: 297.37; Melting point: 144-146° C.; .sup.1H- NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.74 (d, J=9.2 Hz, 2 H), 6.68 (d, J=9.2 Hz, 2 H), 3.49 (dd, J=6.9, 4.2 Hz, 1 H), 3.23 (s, 3 H), 3.06 (s, 6 H), 2.97 (s, 3 H), 2.61 (d, J=4.2 Hz, 1 H), 2.55 (d, J=6.9 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 165.3, 153.6, 130.0, 121.4, 110.8, 40.0, 37.3, 36.0, 35.4, 31.9; LCMS ESI.sup.+ (m/z): 298.2 [M+H].sup.+, LCMS purity 100.00% C-3362 1-(4-Butylphenyl)sulfonyl-N,N-dimethyl-aziridine-2-carboxamide Molecular formula: C.sub.15H.sub.22N.sub.2O.sub.3S; Molecular weight: 310.41; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.86 (d, J=8.4 Hz, 2 H), 7.35 (d, J=8.4 Hz, 2 H), 3.59 (dd, J=6.9, 4.2 Hz, 1 H), 3.22 (s, 3 H), 2.98 (s, 3 H), 2.69 (t, J=7.6 Hz, 2 H), 2.68 (d, J=4.2 Hz, 1 H), 2.65 (d, J=6.9 Hz, 1 H), 1.57-1.66 (m, 2 H), 1.35 (sextet, J=7.5 Hz, 2 H), 0.93 (d, J=7.4 Hz, 3 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 164.9, 150.0, 134.3, 129.2, 128.2, 37.2, 36.0, 35.6, 35.2, 33.1, 32.5, 22.2, 13.8; LCMS ESI.sup.+ (m/z): 311.2 [M+H].sup.+, LCMS purity 100.00% C-3364 1-(4-Isopropylphenyl)sulfonyl-N,N-dimethyl-aziridine-2-carboxamide Molecular formula: C.sub.14H.sub.20N.sub.2O.sub.3S; Molecular weight: 296.38; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.88 (d, J=8.5 Hz, 2 H), 7.40 (d, J=8.5 Hz, 2 H), 3.55 (dd, J=6.9, 4.2 Hz, 1 H), 3.23 (s, 3 H), 3.00 (septet, J=6.9 Hz, 1 H), 2.98 (s, 3 H), 2.69 (d, J=4.2 Hz, 1 H), 2.65 (d, J=6.9 Hz, 1 H), 1.28 (d, J=6.9 Hz, 6H); .sup.13 C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 164.9, 155.8, 134.5, 128.3, 127.3, 37.2, 36.0, 35.2, 34.3, 32.6, 23.6; LCMS ESI.sup.+ (m/z): 297.2 [M+H].sup.+, LCMS purity 100.00% C-3365 N,N-Dimethyl-1-(1-naphthylsulfonyl)aziridine-2-carboxamide Molecular formula: C.sub.15H.sub.16N.sub.2O.sub.3S; Molecular weight: 304.36; Melting point: 110-112° C.; .sup.1H- NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.87 (ddd, J=8.5, 1.8, 0.9 Hz, 1 H), 8.25 (dd, J=7.4, 1.3 Hz, 1 H), 8.15 (dt, J=8.2, 1.2 Hz, 1 H), 7.95 (ddd, J=8.2, 1.3, 0.6 Hz, 1 H), 7.72 (ddd, J=8.5, 6.9, 1.4 Hz, 1 H), 7.63 (ddd, J=8.2, 6.9, 1.2 Hz, 1 H), 7.56 (dd, J=8.2, 7.4 Hz, 1 H), 3.75 (dd, J=6.9, 4.3 Hz, 1 H), 3.20 (s, 3 H), 2.97 (s, 3 H), 2.74 (d, J=6.9 Hz, 1 H), 2.69 (d, J=4.3 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 164.9, 135.6, 134.2, 132.8, 129.7, 129.0, 128.7, 128.7, 127.2, 125.7, 123.9, 37.2, 36.0, 35.8, 32.7; LCMS ESI.sup.+ (m/z): 305.2 [M+H].sup.+, LCMS purity 96.57% C-3366 N,N-Dimethyl-1-[(4-methyl-1-naphthyl)sulfonyl]aziridine-2-carboxamideMolecular formula: C.sub.16H.sub.18N.sub.2O.sub.3S; Molecular weight: 318.39; Melting point: 120-122° C.; .sup.1H- NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.92 (ddd, J=8.3, 1.4, 0.7 Hz, 1 H), 8.14 (d, J=7.6 Hz, 1 H), 8.10 (ddd, J=8.3, 1.3, 0.7 Hz, 1 H), 7.71 (ddd, J=8.3, 6.8, 1.5 Hz, 1 H), 7.66 (ddd, J=8.3, 6.9, 1.5 Hz, 1 H), 7.41 (ddd, J=7.6, 1.9, 0.9 Hz, 1 H), 3.73 (dd, J=6.9, 4.3 Hz, 1 H), 3.20 (s, 3 H), 2.97 (s, 3 H), 2.79 (s, 3 H), 2.70 (d, J=6.9 Hz, 1 H), 2.66 (d, J=4.3 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 164.9, 143.1, 133.3, 130.9, 129.7, 129.0, 128.2, 127.0, 126.2, 124.8, 124.7, 37.3, 35.9, 35.9, 32.6, 20.2; LCMS ESI.sup.+ (m/z): 319.2 [M+H].sup.+, LCMS purity 98.41% C-3368 N,N-Dimethyl-1-(4-pentylphenyl)sulfonyl-aziridine-2-carboxamide Molecular formula: C.sub.16H.sub.24N.sub.2O.sub.3S; Molecular weight: 324.44; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.85 (d, J=8.5 Hz, 2 H), 7.30 (d, J=8.5 Hz, 2 H), 3.59 (dd, J=6.9, 4.3 Hz, 1 H), 3.21 (s, 3 H), 2.97 (s, 3 H), 2.68 (t, J=7.8 Hz, 2 H), 2.68 (d, J=4.3 Hz, 1 H), 2.65 (d, J=6.9 Hz, 1 H), 1.63 (quintet, J=7.5 Hz, 2 H), 1.23-1.39 (m, 4 H), 0.89 (t, J=7.0 Hz, 3 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 164.9, 150.0, 134.4, 129.2, 128.2, 37.2, 36.0, 35.9, 35.2, 32.5, 31.3, 30.7, 22.4, 13.9; LCMS ESI.sup.+ (m/z): 325.2 [M+H].sup.+, LCMS purity 100.00% C-3369 1-(4-Hexylphenyl)sulfonyl-N,N-dimethyl-aziridine-2-carboxamide Molecular formula: C.sub.17H.sub.26N.sub.2O.sub.3S; Molecular weight: 338.46; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.86 (d, J=8.5 Hz, 2 H), 7.34 (d, J=8.5 Hz, 2 H), 3.59 (dd, J=6.9, 4.2 Hz, 1 H), 3.21 (s, 3 H), 2.97 (s, 3 H), 2.68 (t, J=7.8 Hz, 2 H), 2.68 (d, J=4.2 Hz, 1 H), 2.65 (d, J=6.9 Hz, 1 H), 1.62 (quintet, J=7.5 Hz, 2 H), 1.23-1.37 (m, 6 H), 0.88 (t, J=7.0 Hz, 3 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 165.0, 150.0, 134.3, 129.2, 128.2, 37.2, 36.0, 35.9, 35.2, 32.5, 31.6, 30.9, 28.8, 22.5, 14.0; LCMS ESI.sup.+ (m/z): 339.2 [M+H].sup.+, LCMS purity 95.86% C-3371 1-[[5-(Dimethylamino)-1-naphthyl]sulfonyl]-N,N-dimethylaziridine-2-carboxamide Molecular formula: C.sub.17H.sub.21N.sub.3O.sub.3S; Molecular weight: 347.43; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.62 (dt, J=8.5, 1.1 Hz, 1 H), 8.55 (dt, J=8.7, 0.9 Hz, 1 H), 8.23 (dd, J=7.4, 1.3 Hz, 1 H), 7.60 (dd, J=8.7, 7.6 Hz, 1 H), 7.53 (dd, J=8.5, 7.4 Hz, 1 H), 7.21 (dd, J=7.6, 0.9 Hz, 1 H), 3.74 (dd, J=6.9, 4.3 Hz, 1 H), 3.20 (s, 3 H), 2.96 (s, 3 H), 2.88 (s, 6 H), 2.73 (d, J=6.9 Hz, 1 H), 2.68 (d, J=4.3 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 164.9, 151.6, 132.9, 131.8, 130.4, 129.9, 129.7, 128.7, 122.9, 120.1, 115.5, 45.4, 37.3, 35.9, 35.8, 32.7; LCMS ESI.sup.+ (m/z): 348.2 [M+H].sup.+, LCMS purity 95.88 % C-3373 N,N-Dimethyl-1-(2-naphthylsulfonyl)aziridine-2-carboxamide Molecular formula: C.sub.15H.sub.16N.sub.2O.sub.3S; Molecular weight: 304.36; Melting point: oil .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3) δ: 8.54-8.52 (m, 1 H), 8.04-7.90 (m, 4 H), 7.73-7.59 (m, 2 H), 3.67 (dd, J=6.9, 4.3 Hz, 1 H), 3.24 (s, 3 H), 2.98 (s, 3 H), 2.74 (d, J=6.9 Hz, 1 H), 2.72 (d, J=4.3 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 165.0, 135.6, 134.3, 132.1, 129.9, 129.7, 129.6, 128.2, 127.9, 123.1, 37.4, 36.2, 35.5, 32.8 LCMS ESI+ (m/z): 305.2 [M+H]+ , LCMS purity 97.08% C-3374 N,N-Dimethyl-1-[4-(trifluoromethyl)phenyl]sulfonyl-aziridine-2-carboxamide Molecular formula: C.sub.12H.sub.13N.sub.2O.sub.3S; Molecular weight: 322.30; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): 8.12 (d, J=8.4 Hz, 2 H), 7.83 (d, J=8.4 Hz, 2 H), 3.68 (dd, J=6.9, 4.3 Hz, 1 H), 3.25 (s, 3 H), 3.00 (s, 3 H), 2.75 (d, J=4.3 Hz, 1 H), 2.73 (d, J=6.9 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 164.4, 141.1, 135.6 (q, J=33.3 Hz), 128.6, 126.3 (q, J=3.7 Hz), 123.0 (q, J=273.2 Hz), 37.2, 36.0, 35.3, 33.0; LCMS ESI.sup.+ (m/z): 323.1 [M+H].sup.+, LCMS purity 95.04.00% C-3375 Methyl 1-[[6-(dimethylamino)-1-naphthyl]sulfonyl]aziridine-2-carboxylate Molecular formula: C.sub.16H.sub.18N.sub.2O.sub.4S; Molecular weight: 334.39; Melting point: 106-108° C. .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.73 (dt, J=9.5, 0.6 Hz, 1 H), 7.93 (d, J=8.3 Hz, 1 H), 7.89 (dd, J=7.3, 1.2 Hz, 1 H), 7.40 (dd, J=8.3, 7.3 Hz, 1 H), 7.34 (dd, J=9.5, 2.6 Hz,1 H), 6.94 (d, J=2.6 Hz, 1 H), 3.70 (s, 3 H), 3.44 (dd, J=7.1, 4.1 Hz, 1 H),), 3.09 (s, 6 H), 2.83 (d, J=7.1 Hz, 1 H), 2.55 (d, J=4.2 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.3, 148.9, 136.2, 133.8, 132.1, 126.2, 125.6, 124.1, 121.6, 118.2, 106.2, 52.7, 40.4, 35.7, 32.3 LCMS ESI.sup.+ (m/z): 335.1 [M+H].sup.+ , LCMS purity 100% C-3376 Methyl 1-[[6-(dimethylamino)-5-formyl-1-naphthyl]sulfonyl]aziridine-2-carboxylate Molecular formula: C.sub.17H.sub.18N.sub.2O.sub.5S; Molecular weight: 362.40; Melting point: 116-117° C.; .sup.1H- NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 10.30 (s, 1 H), 9.49 (dt, J=8.7, 1.1 Hz, 1 H), 9.02 (dd, J=9.7, 0.9 Hz, 1 H), 8.05 (dd, J=7.4, 1.1 Hz, 1 H), 7.62 (dd, J=8.7, 7.4 Hz, 1 H), 7.53 (d, J=9.7 Hz, 1 H), 3.72 (s, 3 H), 3.47 (dd, J=7.1, 4.1 Hz, 1 H), 3.19 (s, 6 H), 2.85 (d, J=7.1 Hz, 1 H), 2.55 (d, J=4.2 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 190.8, 167.1, 158.1, 133.9, 132.6, 132.0, 131.3, 127.2, 127.0, 123.7, 120.4, 116.4, 52.8, 45.9, 35.8, 32.4; LCMS ESI.sup.+ (m/z): 363.1 [M+H].sup.+, LCMS purity 100.00% C-3377 1-[[6-(Dimethylamino)-1-naphthyl]sulfonyl]-N,N-dimethylaziridine-2-carboxamide Molecular formula: C.sub.17H.sub.21N.sub.3O.sub.3S; Molecular weight: 347.43; Melting point: 147-149° C. .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.72 (d, J=9.5 Hz, 1 H), 7.90 (d, J=8.4 Hz, 1 H), 7.89 (dd, J=7.3, 1.2 Hz, 1 H), 7.49 (dd, J=8.2, 7.5 Hz, 1 H), 7.32 (dd, J=9.5, 2.7 Hz, 1 H), 6.93 (d, J=2.7 Hz, 1 H), 3.67 (dd, J=6.9, 4.3 Hz, 1 H), 3.14 (s, 3 H), 3.08 (s, 6 H), 2.94 (s, 3 H), 2.71 (d, J=6.9 Hz, 1 H), 2.67 (d, J=4.3 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 165.0, 148.9, 136.2, 133.7, 132.3, 126.3, 125.3, 124.1, 121.5, 118.2, 106.1, 40.3, 37.1, 35.9, 35.9, 32.3 LCMS ESI.sup.+ (m/z): 348.1 [M+H]+ , LCMS purity 100% C-3380 1-(4-Hexylphenyl)sulfonyl-N-methyl-aziridine-2-carboxamide Molecular formula: C.sub.16H.sub.24N.sub.2O.sub.3S; Molecular weight: 324.44; Melting point: 84-86° C.; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.83 (d, J=8.5 Hz, 2 H), 7.38 (d, J=8.5 Hz, 2 H), 6.15 (br s, 1 H), 3.28 (dd, J=7.7, 4.2 Hz, 1 H), 2.75 (d, J=4.9 Hz, 3 H), 2.74 (d, J=7.7 Hz, 1 H), 2.71 (t, J=7.8 Hz, 2 H), 2.36 (d, J=4.2 Hz, 1 H), 1.64 (quintet, J=7.5 Hz, 2 H), 1.25-1.39 (m, 6 H), 0.89 (t, J=7.0 Hz, 3 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 166.2, 150.4, 133.4, 129.4, 128.2, 37.9, 36.0, 33.4, 31.5, 30.8, 28.8, 25.9, 22.5, 14.0; LCMS ESI.sup.+ (m/z): 325.1 [M+H].sup.+, LCMS purity 97.38% C-3383 Methyl 1-[[4-(dimethylamino)-1-naphthyl]sulfonyl]aziridine-2-carboxylate Molecular formula: C.sub.16H.sub.18N.sub.2O.sub.4S; Molecular weight: 334.39; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.86 (ddd, J=8.6, 1.3, 0.7 Hz, 1H), 8.23 (ddd, J=8.6, 1.4, 0.7 Hz, 1 H), 8.11 (d, J=8.3 Hz, 1 H), 7.67 (ddd, J=8.6, 6.9, 1.4 Hz, 1 H), 7.56 (ddd, J=8.6, 6.9, 1.3 Hz, 1 H), 6.97 (d, J=8.3 Hz, 1 H), 3.70 (s, 3 H), 3.44 (dd, J=7.1, 4.1 Hz, 1 H), 3.01 (s, 6 H), 2.83 (d, J=7.1 Hz, 1 H), 2.54 (d, J=4.1 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.4, 157.5, 131.3, 130.8, 128.3, 128.2, 125.9, 125.7, 125.3, 124.3, 110.7, 52.7, 44.6, 35.7, 32.4; LCMS ESI.sup.+ (m/z): 335.1 [M+H].sup.+, LCMS purity 100.00% C-3384 1-(4-Cyclohexylphenyl)sulfonyl-N,N-dimethyl-aziridine-2-carboxamide Molecular formula: C.sub.17H.sub.24N.sub.2O.sub.3S; Molecular weight: 336.45; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.86 (d, J=8.5 Hz, 2 H), 7.37 (d, J=8.5 Hz, 2 H), 3.58 (dd, J=6.9, 4.3 Hz, 1 H), 3.21 (s, 3 H), 2.97 (s, 3 H), 2.68 (d, J=4.3 Hz, 1 H), 2.65 (d, J=6.9 Hz, 1 H), 2.54-2.63 (m, 1 H), 1.80-1.92 (m, 4 H), 1.72-1.80 (m, 1 H), 1.32-1.48 (m, 4 H), 1.19-1.32 (m, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 164.9, 154.9, 134.4, 128.2, 127.7, 44.6, 37.3, 36.0, 35.1, 34.0, 32.5, 26.6, 25.9; LCMS ESI.sup.+ (m/z): 337.2 [M+H].sup.+, LCMS purity 95.84% C-3385 1-[[4-(Dimethylamino)-1 -naphthyl] sulfonyl] -N,N-dimethylaziridine-2-carboxamide Molecular formula: C.sub.17H.sub.21N.sub.3O.sub.3S; Molecular weight: 347.43; Melting point: 120-122° C. .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.85 (ddd, J=8.6, 1.3, 0.6 Hz, 1 H), 8.22 (ddd, J=8.6, 1.3, 0.6 Hz, 1 H), 8.12 (d, J=8.2 Hz, 1 H), 7.65 (ddd, J=8.6, 6.9, 1.4 Hz, 1 H), 7.56(ddd, J=8.6, 6.9, 1.4 Hz, 1 H), 6.97 (d, J=8.2 Hz, 1 H), 3.69 (dd, J=6.9, 4.3 Hz, 1 H), 3.20 (s, 3 H), 3.01 (s, 6 H), 2.96 (s, 3 H), 2.68 (d, J=6.9 Hz, 1 H), 2.64 (d, J=4.3 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 165.2, 157.4, 131.0, 130.8, 128.3, 128.2, 126.0, 125.7, 125.3, 124.6, 110.6, 44.6, 37.3, 35.9, 35.8, 32.5 LCMS ESI.sup.+ (m/z): 348.1 [M+H].sup.+ , LCMS purity 100% C-3389 1-(4-Hexylphenyl)sulfonylaziridine-2-carboxamide Molecular formula: C.sub.15H.sub.22N.sub.2O.sub.3S; Molecular weight: 310.41; Melting point: 103-105° C.; .sup.1H-NMR spectrum (400 MHz): (DMSO-d.sub.6, HMDSO) δ: 7.84 (d, J=8.4 Hz, 2 H), 7.81 (br s, 1 H), 7.50 (d, J=8.4 Hz, 2 H), 7.41 (br s, 1 H), 3.23 (dd, J=7.2, 4.3 Hz, 1 H), 2.69 (t, J=7.7 Hz, 2 H), 2.62 (d, J=7.2 Hz, 1 H), 2.46 (d, J=4.3 Hz, 1 H), 1.60 (quintet, J=7.4 Hz, 2 H), 1.22-1.33 (m, 6 H), 0.85 (t, J=7.0 Hz, 3H); .sup.13 C-NMR spectrum (100 MHz): (DMSO-d.sub.6, HMDSO) δ: 167.0, 150.0, 134.5, 129.8, 128.2, 37.1, 35.4, 31.6, 31.4, 30.9, 28.7, 22.4, 14.3; LCMS ESI.sup.+ (m/z): 311.1 [M+H].sup.+, LCMS purity 100.00% C-3390 Methyl 1-[[6-(dimethylamino)-5-formyl-2-naphthyl]sulfonyl]aziridine-2-carboxylate Molecular formula: C.sub.17H.sub.18N.sub.2O.sub.5S; Molecular weight: 362.40; Melting point: 147-149° C. .sup.1H-NMR spectrum (400 MHz): (CDCl3, HMDSO) δ: 10.27 (s, 1 H), 9.22 (d, J=9.1 Hz, 1 H), 8.35 (d, J=2.0 Hz, 1 H), 7.96 (dd, J=9.1, 2.0 Hz, 1 H), 7.94 (d, J=9.1 Hz, 1 H), 7.41 (d, J=9.1 Hz, 1 H), 3.72 (s, 3 H), 3.39 (dd, J=7.1, 4.1 Hz, 1 H), 3.24 (s, 6 H), 2.81 (d, J=7.1 Hz, 1 H), 2.58 (d, J=4.1 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl3, HMDSO) δ: 190.1, 167.2, 159.5, 135.9, 135.7, 131.1, 129.7, 126.5, 126.1, 125.1, 119.6, 115.2, 52.9, 45.7, 35.8, 32.0 LCMS ESI.sup.+ (m/z): 363.1 [M+H].sup.+ , LCMS purity 96.10% C-3391 1-[[6-(Dimethylamino)-5-formyl-2-naphthyl]sulfonyl]-N,N-dimethylaziridine-2-carboxamide Molecular formula: C.sub.18H.sub.21N.sub.3O.sub.4S; Molecular weight: 375.44; Melting point: 58-60° C.; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 10.27 (s, 1 H), 9.21 (dt, J=9.2, 0.6 Hz, 1 H), 8.35 (d, J=2.1 Hz, 1 H), 7.97 (dd, J=9.2, 2.1 Hz, 1 H), 7.94 (d, J=9.2 Hz, 1 H), 7.41 (d, J=9.2 Hz, 1 H), 3.64 (dd, J=6.9, 4.3 Hz, 1 H), 3.24 (s, 3 H), 3.23 (s, 6 H), 2.97 (s, 3 H), 2.70 (d, J=6.9 Hz, 1 H), 2.69 (d, J=4.3 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 190.1, 164.9, 159.5, 135.8, 135.6, 131.5, 129.5, 126.5, 126.1, 125.0, 119.6, 115.2, 45.7, 37.2, 36.0, 35.3, 32.5; LCMS ESI.sup.+ (m/z): 376.1 [M+H].sup.+, LCMS purity 100.00% C-3393 Methyl 1-[[5-chloro-6-(methylamino)-2-naphthyl]sulfonyl]aziridine-2-carboxylate Molecular formula: C.sub.15H.sub.15ClN.sub.2O.sub.4S; Molecular weight: 354.81; Melting point: 170-172° C.; .sup.1H- NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.36 (d, J=1.9 Hz, 1 H), 8.12 (dt, J=9.1, 0.6 Hz, 1 H), 7.90 (dd, J=9.1, 2.0 Hz, 1 H), 7.83 (d, J=9.0 Hz, 1 H), 7.19 (d, J=9.0 Hz, 1 H), 5.01 (q, J=5.1 Hz, 1 H), 3.72 (s, 3 H), 3.39 (dd, J=7.1, 4.1 Hz, 1 H), 3.09 (d, J=5.1 Hz, 3 H), 2.81 (d, J=7.1 Hz, 1 H), 2.56 (d, J=4.1 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.3, 145.4, 133.9, 130.5, 129.7, 129.1, 125.3, 124.4, 123.3, 114.3, 110.5, 52.8, 35.7, 32.0, 30.3; LCMS ESI.sup.+ (m/z): 355.0 [M+H].sup.+, LCMS purity 100.00% C-3397 Methyl 1-[[6-(dimethylamino)-2-naphthyl]sulfonyl]aziridine-2-carboxylate Molecular formula: C.sub.16H.sub.18N.sub.2O.sub.4S; Molecular weight: 334.39; Melting point: 156-158° C.; .sup.1H- NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.31 (d, J=1.9 Hz, 1 H), 7.92 (d, J=9.2 Hz, 1 H), 7.77 (dd, J=8.8, 1.9 Hz, 1 H), 7.71 (d, J=8.8 Hz, 1 H), 7.22 (dd, J=9.2, 2.6 Hz, 1 H), 6.88 (d, J=2.6 Hz, 1 H), 3.72 (s, 3 H), 3.36 (dd, J=7.1, 4.1 Hz, 1 H), 3.13 (s, 6 H), 2.78 (d, J=7.1 Hz, 1 H), 2.56 (d, J=4.1 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.4, 150.7, 137.7, 130.5, 130.0, 128.1, 127.0, 124.4, 123.4, 116.3, 104.9, 52.8, 40.3, 35.6, 32.0; LCMS ESI.sup.+ (m/z): 335.1 [M+H].sup.+, LCMS purity 100.00% C-3398 1-[[6-(Dimethylamino)-2-naphthyl]sulfonyl]-N,N-dimethylaziridine-2-carboxamide Molecular formula: C.sub.17H.sub.21N.sub.3O.sub.3S; Molecular weight: 347.43; Melting point: foam; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.31 (d, J=2.0 Hz, 1 H), 7.79 (d, J=9.2 Hz, 1 H), 7.78 (dd, J=8.7, 2.0 Hz, 1 H), 7.71 (d, J=8.7 Hz, 1 H), 7.21 (dd, J=9.2, 2.5 Hz, 1 H), 6.87 (d, J=2.5 Hz, 1 H), 3.59 (dd, J=6.9, 4.3 Hz, 1 H), 3.21 (s, 3 H), 3.12 (s, 6 H), 2.96 (s, 3 H), 2.68 (d, J=4.3 Hz,1 H), 2.67 (d, J=6.9 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 165.1, 150.6, 137.6, 130.4, 129.8, 128.5, 127.0, 124.4, 123.4, 117.0, 105.0, 40.3, 37.3, 36.0, 35.4, 32.3; LCMS ESI.sup.+ (m/z): 348.1 [M+H].sup.+, LCMS purity 96.37% C-3399 Methyl 1-[[5-(dimethylamino)-2-naphthyl]sulfonyl]aziridine-2-carboxylate Molecular formula: C.sub.16H.sub.18N.sub.2O.sub.4S; Molecular weight: 334.39; Melting point: 85-87° C. .sup.1H-NMR spectrum (400 MHz): (CDCl3, HMDSO) δ: 8.47 (d, J=2.0 Hz, 1 H), 8.40 (dt, J=9.0, 0.7 Hz, 1 H), 7.93 (dd, J=9.0, 2.0 Hz, 1 H), 7.63 (dt, J=8.2, 1.0 Hz, 1H), 7.54 (dd, J=8.2, 7.6 Hz, 1 H), 7.25 (dd, J=7.6, 1.0 Hz, 1 H), 3.73 (s, 3 H), 3.43 (dd, J=7.1, 4.1 Hz, 1 H), 2.90 (s, 6 H), 2.84 (d, J=7.1 Hz, 1 H), 2.60 (d, J=4.1 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl3, HMDSO) 167.2, 151.1, 133.6, 133.5, 131.1, 130.2, 127.8, 126.2, 123.9, 121.9, 117.4, 52.9, 45.1, 35.8, 32.1 LCMS ESI.sup.+ (m/z): 335.1 [M+H].sup.+ , LCMS purity 100% C-3400 1-[[5-(Dimethylamino)-2-naphthyl]sulfonyl]-N,N-dimethylaziridine-2-carboxamide Molecular formula: C.sub.17H.sub.21N.sub.3O.sub.3S; Molecular weight: 347.43; Melting point: 96-98° C.; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.47 (d, J=1.9 Hz, 1 H), 8.39 (dt, J=9.0, 0.7 Hz, 1 H), 7.94 (dd, J=9.0, 1.9 Hz, 1 H), 7.62 (dt, J=8.2, 1.0 Hz, 1 H), 7.53 (dd, J=8.2, 7.6 Hz, 1 H), 7.24 (dd, J=7.6, 1.0 Hz, 1 H), 3.67 (dd, J=6.9, 4.3 Hz, 1 H), 3.25 (s, 3 H), 2.98 (s, 3 H), 2.90 (s, 6 H), 2.73 (d, J=6.9 Hz, 1 H), 2.72 (d, J=4.3 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) 167.9, 151.1, 133.9, 133.4, 131.0, 130.0, 127.8, 126.1, 123.8, 122.0, 117.3, 45.1, 37.3, 36.0, 35.3, 32.6; LCMS ESI.sup.+ (m/z): 348.2 [M+H].sup.+, LCMS purity 100.00% C-3402 1-(2,4-Difluorophenyl)sulfonylaziridine-2-carboxamide Molecular formula: C.sub.9H.sub.8F.sub.2NO.sub.3 S; Molecular weight: 262.23; Melting point: 141-143° C.; .sup.1H- NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) 7.99 (dt, J=8.5, 6.2 Hz, 1 H), 7.87 (s, 1 H), 7.66-7.74 (m, 1 H), 7.47 (s, 1 H), 7.36-7.43 (m, 1 H), 3.38 (dd, J=7.2, 4.5 Hz, 1 H), 2.77 (d, J=7.2 Hz, 1 H), 2.59 (d, J=4.5 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) 166.6, 166.7 (dd, J=256.9, 12.1 Hz,), 160.5 (dd, J=258.8, 13.7 Hz,), 132.8 (d, J=11.1 Hz,), 122.2 (dd, J=14.6, 3.7 Hz,), 113.3 (dd, J=22.4, 3.4 Hz,), 107.0 (t, J=26.4 Hz,), 37.3, 32.3; LCMS ESI.sup.+ (m/z): 263.1 [M+H].sup.+, LCMS purity 100.00% C-3403 1-(2,4-Difluorophenyl)sulfonyl-N,N-dimethyl-aziridine-2-carboxamide Molecular formula: C.sub.11H.sub.12F.sub.2NO.sub.3S; Molecular weight: 290.29; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) 7.99 (ddd, J=8.8, 7.8, 6.0 Hz, 1 H), 6.96-7.06 (m, 2 H), 3.26 (s, 3 H), 2.99 (s, 3 H), 3.71 (dd, J=7.0, 4.4 Hz, 1 H), 2.88 (d, J=7.0 Hz, 1 H), 2.81 (d, J=4.4 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 166.7 (dd, J=259.4, 11.6 Hz,), 164.5, 160.5 (dd, J=260.8, 13.1 Hz,), 132.3 (d, J=10.9 Hz,), 122.3 (dd, J=14.6, 3.8 Hz,), 112.1 (dd, J=22.2, 3.4 Hz,), 106.0 (t, J=25.6 Hz,), 37.2, 36.1, 35.1, 33.4; LCMS ESI.sup.+ (m/z): 291.1 [M+H].sup.+, LCMS purity 94.31% C-3427 Methyl 1-[[8-(dimethylamino)-2-naphthyl]sulfonyl]aziridine-2-carboxylate Molecular formula: C.sub.16H.sub.18N.sub.2O.sub.4S; Molecular weight: 334.39; Melting point: oil; .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.88-8.89 (m, 1 H), 7.96 (dd, J=8.8, 0.7 Hz, 1 H), 7.92 (dd, J=8.8, 1.8 Hz, 1 H), 7.58 (dd, J=8.2, 6.7 Hz, 1 H), 7.55 (ddd, J=8.2, 1.8, 0.7 Hz, 1 H), 7.17 (dd, J=6.7, 1.8 Hz, 1 H), 3.72 (s, 3 H), 3.42 (dd, J=7.1, 4.1 Hz, 1 H), 2.92 (s, 6 H), 2.84 (d, J=7.1 Hz, 1 H), 2.59 (d, J=4.1 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) 167.2, 152.6, 137.1, 132.8, 129.9, 129.7, 127.6, 126.8, 122.8, 122.2, 115.7, 52.8, 45.2, 35.8, 32.1; LCMS ESI.sup.+ (m/z): 335.2 [M+H].sup.+, LCMS purity 100.00% C-3459 1-[[6-(Dimethylamino)-1-naphthyl]sulfonyl]aziridine-2-carboxamide Molecular formula: C.sub.15H.sub.17N.sub.3O.sub.3S; Molecular weight: 319.38; Melting point: 197-199° C. .sup.1H-NMR spectrum (300 MHz): (DMSO-D.sub.6, HMDSO) δ: 8.55 (d, J=9.6 Hz, 1 H), 8.07 (d, J=8.3 Hz, 1 H), 7.80 (dd, J=7.3, 1.0 Hz, 1 H), 7.76 (br s, 1 H), 7.51 (dd, J=8.3, 7.3 Hz, 1 H), 7.45 (dd, J=9.6, 2.7 Hz, 1 H), 7.37 (br s, 1 H), 7.11 (d, J=2.7 Hz, 1 H), 3.28-3.38 (m, overlapped with water, 1 H), 3.09 (s, 6 H), 2.68 (d, J=7.2 Hz, 1 H), 2.47 (d, J=4.4 Hz, 1 H); .sup.13C-NMR spectrum(100 MHz): (DMSO-D.sub.6, HMDSO) δ: 171.8, 154.0, 141.2, 138.8, 137.3, 130.9, 130.0, 129.7, 125.7, 123.3, 111.3, 45.8, 41.2, 36.9; LCMS ESI.sup.+ (m/z): 320.3 [M+H].sup.+ , LCMS purity 100% C-3511 [1-(4-Hexylphenyl)sulfonylaziridin-2-yl]-pyrrolidin-1-yl-methanone Molecular formula: C.sub.19H.sub.28N.sub.2O.sub.3S; Molecular weight: 364.50; Melting point: oil .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.85 (d, J=8.3 Hz, 2 H), 7.34 (d, J=8.3 Hz, 2 H), 3.75 (dt, J=10.1, 6.7 Hz, 1 H), 3.63 (dt, J=10.1, 7.0 Hz, 1 H), 3.42-3.54 (m, 3 H), 2.70 (d, J=4.2 Hz, 1 H), 2.68 (t, J=7.9 Hz, 2 H), 2.64 (d, J=6.9 Hz, 1 H), 1.93-2.05 (m, 2 H), 1.81-1.93 (m, 2 H), 1.57-1.69 (m, 2 H), 1.23-1.38 (m, 6 H), 0.88 (t, J=7.0 Hz, 3 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 163.4, 150.0, 134.4, 129.2, 128.3, 46.8, 46.5, 36.0, 35.8, 32.4, 31.6, 31.0, 28.9, 26.1, 24.2, 22.6, 14.1; LCMS ESI.sup.+ (m/z): 365.3 [M+H].sup.+ , LCMS purity 100% C-3517 [1-(4-Hexylphenyl)sulfonylaziridin-2-yl]-morpholino-methanone Molecular formula: C.sub.19H.sub.28N.sub.2O.sub.4S; Molecular weight: 380.18; Melting point: oil .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.85 (d, J=8.4 Hz, 2 H), 7.36 (d, J=8.4 Hz, 2 H), 3.75-3.86 (m, 2 H), 3.57-3.75 (m, 5 H), 3.55 (dd, J=6.8, 4.2 Hz, 1 H), 3.46 (ddd, J=13.3, 7.7, 3.3 Hz, 1 H), 2.71 (d, J=4.2 Hz, 1 H), 2.69 (t, J=7.9 Hz, 2 H), 2.67 (d, J=6.8 Hz, 1 H), 1.57-1.68 (m, 2 H), 1.23-1.39 (m, 6 H), 0.88 (t, J=7.0 Hz, 3 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 163.7, 150.3, 134.3, 129.3, 128.2, 66.7, 66.6, 42.8, 36.0, 35.3, 32.4, 31.6, 31.0, 28.9, 22.7, 14.1; LCMS ESI.sup.+ (m/z): 381.3 [M+H].sup.+ , LCMS purity 100% C-3520 [1-(4-hexylphenyl)sulfonylaziridin-2-yl]-(1-piperidyl)methanone Molecular formula: C.sub.20H.sub.30N.sub.2O.sub.3S; Molecular weight: 378.53; Melting point: oil .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.86 (d, J=8.4 Hz, 2 H), 7.35 (d, J=8.4 Hz, 2 H), 3.62-3.73 (m, 2 H), 3.54 (dd, J=6.8, 4.2 Hz, 1 H), 3.52-3.60 (m, 1 H), 3.38-3.46 (m, 1 H), 2.69 (t, J=7.3 Hz, 2 H), 2.70 (d, J=4.2 Hz, 1 H), 2.66 (d, J=6.8 Hz, 1 H), 1.60-1.70 (m, 4 H), 1.49-1.60 (m, 4 H), 1.24-1.38 (m, 6 H), 0.88 (t, J=7.0 Hz, 3 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 163.3, 150.0, 134.6, 129.2, 128.2, 46.9, 43.6, 36.0, 35.7, 32.3, 31.6, 31.0, 28.9, 26.4, 25.4, 24.4, 22.6, 14.1; LCMS ESI.sup.+ (m/z): 379.3 [M+H].sup.+ , LCMS purity 100% C-3532 1-(Benzenesulfonyl)aziridine-2-carboxamide Molecular formula: C.sub.9H.sub.10N.sub.2O.sub.3S; Molecular weight: 226.25; Melting point: 108-110° C. .sup.1H- NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.93-7.98 (m, 2 H), 7.67-7.73 (m, 1 H), 7.55-7.63 (m, 2 H), 6.11 (s, 1 H), 5.82 (s, 1 H), 3.28 (dd, J=7.7, 4.2 Hz, 1 H), 2.81 (d, J=7.7 Hz, 1 H), 2.45 (d, J=4.2 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 168.3, 136.6, 134.4, 129.5, 128.2, 37.7, 33.2; LCMS ESI.sup.+ (m/z): 227.2 [M+H].sup.+ , LCMS purity 100.00% C-3535 Methyl (2S)-1-(p-tolylsulfonyl)aziridine-2-carboxylate Molecular formula: C.sub.11H.sub.13NO.sub.4S; Molecular weight: 255.29. Melting point: oil. .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.84 (d, J=8.3 Hz, 2 H), 7.36 (d, J=8.3 Hz, 2 H), 3.74 (s, 3 H), 3.34 (dd, J=7.1, 4.1 Hz, 1 H), 2.76 (d, J=7.1 Hz, 1 H), 2.56 (d, J=4.1 Hz, 1 H), 2.45 (s, 3 H). .sup.13C-NMR spectrum (100 MHz (CDCl.sub.3, HMDSO) δ: 167.2, 145.3, 134.0, 129.9, 128.2, 52.9, 35.7, 32.0, 21.7. LCMS ESI.sup.+ (m/z): 256.1 [M+H].sup.+ , LCMS purity 100% C-3537 Ethyl 1-(p-tolylsulfonyl)aziridine-2-carboxylate Molecular formula: C.sub.12H.sub.15NO.sub.4S. Molecular weight: 269.32. Melting point: oil. .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.85 (d, J=8.3 Hz, 2 H), 7.35 (d, J=8.3 Hz, 2 H), 4.12-4.24 (m, 2 H), 3.32 (dd, J=7.1, 4.1 Hz, 1 H), 2.75 (d, J=7.1 Hz, 1 H), 2.55 (d, J=4.1 Hz, 1 H), 2.45 (s, 3 H), 1.25 (t, J=7.1 Hz, 3 H). .sup.13C-NMR spectrum (100 MHz (CDCl.sub.3, HMDSO) δ: 166.8, 145.2, 134.1, 130.0, 128.3, 62.1, 35.9, 32.0, 21.7, 14.0. LCMS ESI.sup.+ (m/z): 270.2 [M+H].sup.+ , LCMS purity 100% C-3539 Methyl (2R)-1-(p-tolylsulfonyl)aziridine-2-carboxylate Molecular formula: C.sub.11H.sub.13NO.sub.4S; Molecular weight: 255.29. Melting point: oil. .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.84 (d, J=8.3 Hz, 2 H), 7.36 (d, J=8.3 Hz, 2 H), 3.74(s, 3 H), 3.34 (dd, J=7.1, 4.1 Hz, 1 H), 2.76 (d, J=7.1 Hz, 1 H), 2.56 (d, J=4.1 Hz, 1 H), 2.45 (s, 3 H). .sup.13C-NMR spectrum (100 MHz (CDCl.sub.3, HMDSO) δ: 167.2, 145.3, 134.0, 129.9, 128.2, 52.9, 35.7, 32.0, 21.7. LCMS ESI.sup.+ (m/z): 256.1 [M+H].sup.+ , LCMS purity 100%. .sup.13C-NMR spectrum (100 MHz (CDCl.sub.3, HMDSO) δ: 167.3, 145.3, 134.0, 130.0, 128.3, 53.0, 35.7, 32.1, 21.7. LCMS ESI.sup.+ (m/z): 256.1 [M+H].sup.+ , LCMS purity 97.75% C-3546 N,N-Diethyl-1-(4-hexylphenyl)sulfonyl-aziridine-2-carboxamide Molecular formula: C.sub.19H.sub.30N.sub.2O.sub.3S; Molecular weight: 366.52; Melting point: oil .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.86 (d, J=8.4 Hz, 2 H), 7.34 (d, J=8.4 Hz, 2 H), 3.56 (dq, J=15.0, 7.2 Hz, 1 H), 3.54 (dd, J=6.8, 4.2 Hz, 1 H), 3.49 (dq, J=15.0, 7.2 Hz, 1 H), 3.32-3.44 (m, 2 H), 2.69 (d, J=4.2 Hz, 1 H), 2.69 (t, J=7.9 Hz, 2 H), 2.65 (d, J=6.9 Hz, 1 H), 1.56-1.67 (m, 2 H), 1.26-1.38 (m, 6 H), 1.26 (t, J=7.2 Hz, 3 H), 1.13 (t, J=7.2 Hz, 3 H), 0.89 (t, J=7.0 Hz, 3 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 164.3, 150.0, 134.5, 129.2, 128.2, 42.1, 41.1, 36.0, 34.9, 32.5, 31.6, 31.0, 28.8, 22.6, 14.7, 14.1, 12.8; LCMS ESI.sup.+ (m/z): 367.3 [M+H].sup.+ , LCMS purity 100% C-3548 Methyl (2S)-1-[[6-(dimethylamino)-1-naphthyl]sulfonyl]aziridine-2-carboxylate Molecular formula: C.sub.16H.sub.18N.sub.2O.sub.4S; Molecular weight: 334.39; Melting point: 118-120° C. .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.73 (d, J=9.6 Hz, 1 H), 7.91 (d, J=8.3 Hz, 1 H), 7.87 (dd, J=7.3, 1.2 Hz, 1 H), 7.39 (dd, J=8.3, 7.4 Hz, 1 H), 7.33 (dd, J=9.6, 2.7 Hz, 1 H), 6.93 (d, J=2.7 Hz, 1 H), 3.70 (s, 3 H), 3.44 (dd, J=7.1, 4.1 Hz, 1 H),), 3.08 (s, 6 H), 2.83 (d, J=7.1 Hz, 1 H), 2.55 (d, J=4.2 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.3, 148.9, 136.2, 133.8, 132.0, 126.2, 125.6, 124.1, 121.5, 118.2, 106.2, 52.8, 40.4, 35.7, 32.3. LCMS ESI.sup.+ (m/z): 335.2 [M+H].sup.+ , LCMS purity 100% C-3559 Methyl 1-(3-pyridylsulfonyl)aziridine-2-carboxylate Molecular formula: C.sub.9H.sub.10N.sub.2O.sub.4S; Molecular weight: 242.25; Melting point: oil .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 9.17 (dd, J=2.3, 0.7 Hz, 1 H), 8.90 (dd, J=4.9, 1.6 Hz, 1 H), 8.28 (ddd, J=8.1, 2.3, 1.7 Hz, 1 H), 7.53 (ddd, J=8.1, 4.9, 0.7 Hz, 1 H), 3.76 (s, 3 H), 3.45 (dd, J=7.1, 4.2 Hz, 1 H), 2.87 (d, J=7.1 Hz, 1 H), 2.65 (d, J=4.2 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 166.88, 154.7, 148.8, 135.9, 134.2, 124.1, 53.1, 36.0, 32.4; LCMS ESI.sup.+ (m/z): 243.1 [M+H].sup.+ , LCMS purity 92.21% C-3562 1-(3-pyridylsulfonyl)aziridine-2-carboxamide Molecular formula: C.sub.8H.sub.9N.sub.3O.sub.3S; Molecular weight: 227.24; Melting point: 147-149° C. .sup.1H-NMR spectrum (400 MHz): (DMSO-D.sub.6, HMDSO) δ: 9.11 (dd, J=2.3, 0.7 Hz, 1 H), 8.96 (dd, J=4.9, 1.6 Hz, 1 H), 8.38 (ddd, J=8.1, 2.3, 1.6 Hz, 1 H), 7.87 (s, 1 H), 7.53 (ddd, J=8.1, 4.9, 0.7 Hz, 1 H), 7.46 (s, 1 H), 3.34-3.38 (m, 1 H, overlapped with H.sub.2O), 2.77 (d, J=7.2 Hz, 1 H), 2.56 (d, J=4.5 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (DMSO-D.sub.6, HMDSO) δ: 166.69, 155.3, 148.5, 136.4, 134.1, 125.1, 37.6, 32.0; LCMS ESI.sup.+ (m/z): 228.1 [M+H].sup.+ , LCMS purity 100% C-3570 Methyl (2R)-1-[[6-(dimethylamino)-1-naphthyl]sulfonyl]aziridine-2-carboxylate Molecular formula: C.sub.16H.sub.18N.sub.2O.sub.4S; Molecular weight: 334.39; Melting point: 117-119° C. .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 8.73 (d, J=9.5 Hz, 1 H), 7.91 (d, J=8.3 Hz, 1 H), 7.87 (dd, J=7.3, 1.2 Hz, 1 H), 7.39 (dd, J=8.3, 7.4 Hz, 1 H), 7.33 (dd, J=9.5, 2.7 Hz, 1 H), 6.93 (d, J=2.7 Hz, 1 H), 3.70 (s, 3 H), 3.44 (dd, J=7.1, 4.1 Hz, 1 H),), 3.08 (s, 6 H), 2.83 (d, J=7.1 Hz, 1 H), 2.55 (d, J=4.2 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.4, 148.9, 136.3, 133.8, 132.0, 126.2, 125.6, 124.2, 121.6, 118.2, 106.3, 52.8, 40.4, 35.7, 32.4; LCMS ESI.sup.+ (m/z): 335.3 [M+H].sup.+ , LCMS purity 100% C-3576 Methyl 1-(4-fluorophenyl)sulfonylaziridine-2-carboxylate Molecular formula: C.sub.10H.sub.10FNO.sub.4S; Molecular weight: 259.25; Melting point: oil .sup.1H-NMR spectrum (400 MHz): (CDCl.sub.3, HMDSO) δ: 7.96-8.02 (m, 2 H), 7.21-7.27 (m, 2 H), 3.74 (s, 3 H), 3.37 (dd, J=7.1, 4.1 Hz, 1 H), 2.79 (d, J=7.1 Hz, 1 H), 2.59 (d, J=4.1 Hz, 1 H); .sup.13C-NMR spectrum (100 MHz): (CDCl.sub.3, HMDSO) δ: 167.1, 166.1 (d, J=257.1 Hz, 1 H), 133.2 (d,J=3.1 Hz, 1 H), 131.1 (d, J=9.9 Hz, 1 H), 116.7 (d, J=22.9 Hz, 1 H), 53.0, 35.9, 32.2; LCMS ESI.sup.+ (m/z): 260.2 [M+H].sup.+, LCMS purity 100% C-3591 1-(4-tert-Butylphenyl)sulfonylaziridine-2-carboxamide Molecular formula: C.sub.13H.sub.18N.sub.2O.sub.3S. Molecular weight: 282.36. Melting point: 151-153° C. .sup.1H- NMR spectrum (400 MHz): (CDC1.sub.3, HMDSO) δ: 7.86 (d, J=8.8 Hz, 2 H), 7.59 (d, J=8.8 Hz, 2 H), 6.07 (br s, 1 H), 5.42 (br s, 1 H), 3.24 (dd, J=7.7, 4.2 Hz, 1 H), 2.81 (d, J=7.7 Hz, 1 H), 2.44 (d, J=4.2 Hz, 1 H), 1.36 (s, 9 H). .sup.13C-NMR spectrum (100 MHz (CDC1.sub.3, HMDSO) δ: 168.4, 158.5, 133.2, 128.1, 126.5, 37.6, 35.4, 33.2, 31.4. LCMS ESI.sup.+ (m/z): 283.3 [M+H].sup.+, LCMS purity 100% C-3593 1-(4-tert-Butylphenyl)sulfonyl-N-methylaziridine-2-carboxamide Molecular formula: C.sub.14H.sub.20N.sub.2O.sub.3S. Molecular weight: 296.38. Melting point: 146-148° C. .sup.1H- NMR spectrum (400 MHz): (CDC1.sub.3, HMDSO) δ: 7.85 (d, J=8.7 Hz, 2 H), 7.59 (d, J=8.7 Hz, 2 H), 6.16 (br s, 1 H), 3.28 (dd, J=7.7, 4.2 Hz, 1 H), 2.76 (d, J=4.9 Hz, 3 H), 2.73 (d, J=7.7 Hz, 1 H), 2.36 (d, J=4.2 Hz, 1 H), 1.36 (s, 9 H). .sup.13C-NMR spectrum (100 MHz (CDC1.sub.3, HMDSO) δ: 166.3, 158.5, 133.1, 128.2, 126.5, 37.9, 35.4, 33.5, 31.0, 26.0. LCMS ESI.sup.+ (m/z): 297.3 [M+H].sup.+ , LCMS purity 100% C-3594 1-(4-tert-Butylphenyl)sulfonyl-N,N-dimethyl-aziridine-2-carboxamide Molecular formula: C.sub.15H.sub.22N.sub.2O.sub.3S. Molecular weight: 310.41. Melting point: 104-106° C. .sup.1H- NMR spectrum (400 MHz): (CDC1.sub.3, HMDSO) δ: 7.88 (d, J=8.6 Hz, 2 H), 7.56 (d, J=8.6 Hz, 2 H), 3.23 (s, 3 H), 3.60 (dd, J=6.8, 4.2 Hz, 1 H), 3.23 (s, 3 H), 2.98 (s, 3 H), 2.69 (d, J=6.8 Hz, 1 H), 2.66 (d, J=4.2 Hz, 1 H), 1.35 (s, 9 H). .sup.13C-NMR spectrum (100 MHz (CDC1.sub.3, HMDSO) δ: 165.0, 159.1, 134.2, 128.0, 126.3, 37.3, 36.0, 35.3, 35.2, 31.1. LCMS ESI.sup.+ (m/z): 311.3 [M+H].sup.+ , LCMS purity 100% C-3612 Lithium 1-tosylaziridine-2-carboxylate Molecular formula: C.sub.10H.sub.10LiNO.sub.4S; Molecular weight: 247.20; Melting point: 222-224° C. (decomp.) .sup.1H-NMR spectrum (400 MHz): (D.sub.2O, HMDSO) d: 7.84 (d, J=8.3 Hz, 2 H), 7.49 (d, J=8.3 Hz, 2 H), 3.10 (dd, J=7.1, 4.1 Hz, 1 H), 2.74 (d, J=7.1 Hz, 1 H), 2.51 (d, J=4.1 Hz, 1 H), 2.44 (s, 3H); .sup.13C-NMR spectrum (100 MHz): (D.sub.2O, HMDSO) d: 173.2, 146.7, 131.6, 130.2, 127.9, 39.0, 32.3, 20.8.LCMS ESI.sup.- (m/z): 240.2 [M-Li].sup.-, LCMS purity 95.83%

Example 2 Inhibition of PDI A1

[0086] The inhibitory effects compounds of invention on activity of PDI A1 was assess based on the insulin turbidometric assay. Enzymatic activity of PDIA1 was confirmed by measuring the turbidity increase at 650 nm due to insulin reduction. The assay mixture was prepared by addition 10 ug/ml PDIA1 (E.coli recombinant protein; Mybiosource), 0.1 mM phosphate buffer (pH7.6), 1 mM EDTA, 0.087 mM DTT and with or without tested compound and was incubated for 60 min, at 37° C. Reaction was started by addition insulin and DTT. Final concentration of insulin and DTT in assay mixture was 0.15 mM and 0.174 mM, respectively. Turbidity was detected at 650 nm against reference samples without PDI A1s. The measurements were performed at 650 nm using 120-s recordings.

TABLE-US-00002 Inhibition of PDI A1 Compound Number Inhibition of PDI A1 (EC .sub.50, .Math.M) Compound Number Inhibition of PDI A1(EC .sub.50, .Math.M) Compound Number Inhibition of PDI A1(EC .sub.50, .Math.M) C-3389 0,03 C-3385 0,7 C-3294 8,4 C-3380 0,033 C-3270 0,8 C-3403 12,3 C-3369 0,04 C-3427 0,94 C-3402 12,3 C-3287 0,05 C-3373 0,95 C-3303 12,6 C-3257 0,08 C-3271 1 C-3343 16 C-3368 0,085 C-3329 1,1 C-3308 18 C-3399 0,12 C-3316 1,2 C-3520 18,5 C-3384 0,12 C-3398 1,4 C-3297 18,6 C-3281 0,14 C-3332 1,4 C-3324 21,5 C-3376 0,24 C-3366 1,5 C-3320 22,8 C-3400 0,25 C-3326 1,5 C-3537 25 C-3383 0,25 C-3327 2,2 C-3594 26 C-3377 0,26 C-3319 2,4 C-3593 29 C-3375 0,29 C-3365 2,6 C-3576 29 C-3393 0,34 C-3273 3 C-3562 29 C-3391 0,35 C-3314 4,1 C-3539 29 C-3295 0,35 C-3296 4,4 C-3357 30 C-3290 0,4 C-3161 5 C-3532 31 C-3291 0,4 C-3311 5 C-3459 33 C-3288 0,4 C-3353 5 C-3342 33,4 C-3371 0,48 C-3350 5,5 C-3212 34 C-3362 0,5 C-3305 5,6 C-3612 54,4 C-3272 0,5 C-3548 6 C-3216 56 C-3292 0,5 C-3251 6 C-3511 72,5 C-3256 0,5 C-3304 6,8 C-3263 140 C-3336 0,53 C-3355 7,7 C-3262 160 C-3397 0,57 C-3559 10,6 C-3346 >200 C-3390 0,6 C-3570 11 C-3220 >200 C-3374 0,65 C-3591 11 C-3218 >200 C-3364 0,7 C-3535 11,2 C-3299 0,8 C-3517 12,1

Example 3. The in Vitro Antiproliferative Effect of PDI A1inhibitors Toward Panel of Cancer Cells (48-hour Exposition)

[0087] Anticancer activity of compounds of invention, PDI A1-inhibitors has been tested in vitro in classical antiproliferative assay in various cancer cells lines Monolayer tumor cell lines MDA-MB-231 (human mammary breast adenocarcinoma), MCF-7 (human breast adenocarcinoma, estrogen-positive), HT-1080 (human fibrosarcoma) and Caco-2 (human colon adenocarcinoma) were cultured in standard medium DMEM (Dulbecco’s modified Eagle’s medium) (“Sigma”) supplemented with 10% fetal bovine serum (“Sigma”). About 2000-4000 cells per well (depending on line nature) were placed in 96-well plates and after 24 h compounds were added to the wells. Untreated cells were used as a control. The plates were incubated for 48 h, 37° C., 5% CO.sub.2. The number of surviving cells was determined using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolinium bromide (MTT). MTT-test: after incubating culture medium was removed and 200 .Math.L fresh medium with 20 .Math.L MTT (2 mg/mL in HBSS) was added in each well of the plate. After incubation (3 hr., 37° C., 5% CO.sub.2), the medium with MTT was removed and 200 .Math.L DMSO were added at once to each sample. The samples were tested at 540 nm on Thermo Scientific Multiskan EX microplate photometer. The half-maximal inhibitory concentration (IC.sub.50) of each compound was calculated using Graph Pad Prism® 3.0. The results are presented in Table 5.

TABLE-US-00003 The in vitro antiproliferative effect of PDI A1inhibitors towards panel of cancer cells (48-hour exposition) Comp. Cytotoxicity, IC.sub.50, .Math.M HT-1080 CaCo-2 MDA-MB-231 MCF-7 C-3212 56±9 45±4 46±8 54±4 C-3216 15±2 40±5 22±1 16±0.2 C-3218 200±3 200±1 64±5 137±14 C-3220 5.9±1.1 56±4 45±9 35±6 C-3256 215±5 205±29 8.9±1.6 2.8±3.2 C-3262 3.8±0.3 13.5±0.8 6.8±0.8 7.2±0.8 C-3263 7.6±0.2 29±0.8 9.1±0.5 17±0.2 C-3270 21±3 87±4 52±5 33±4 C-3271 49±6 138±11 13±2 54±4 C-3272 4.5±0.9 57±6 8.4±0.9 26±0.4 C-3273 31±0.9 56±12 35±3 92±2 C-3281 164±3.2 125±6.4 15±1 118±5 C-3287 92±9.2 144±6 12±2 123±17 C-3288 70±2.9 118±3 10±1 113±4 C-3290 9.5±1.8 6.9±0.2 7.8±1.6 29±4 C-3291 140±3 140±5 32±4 34±1 C-3292 34±3.4 14.4±1.4 16±1 25±1 C-3294 88.5±11 8.1±0.7 40±6 49±6 C-3295 74.1±2.5 12±1.1 17±1 32±2 C-3296 210±15 37±1.5 30±1 32±1 C-3297 154±11 15.4±0.7 5.6±0.6 7.5±0.5 C-3299 56±3 53±7 18±2 41±2 C-3303 70±2 27±2 102±9 170±35 C-3304 17±3 10±1 13±1 49±1 C-3305 190±3 21±1 12±1 25±1 C-3308 120±6 100±5 >500 485±32 C-3311 5.1±0.2 7.2±0.2 33±4 124±5 C-3314 4.5±1 14±0.8 104±3 206±21 C-3316 76±3 81±4 78±12 137±18 C-3319 44±4 31±6 25±5 28±8 C-3320 180±8 78±19 380±15 >500 C-3324 510±3 27±3 102±12 156±9 C-3326 100±5 170±20 169±20 349±13 C-3327 130±10 150±10 161±2 168±23 C-3329 33±4 19±2 6.5±0.5 8.2±0.8 C-3332 140±20 5.9±0.3 44±7 28±3 C-3336 4.6±0.4 0.5±0.1 7.6±1.9 16±3 C-3342 6.7±2 6±0.5 17±2 33±2 C-3343 6.5±0.6 68±4 26±8 46±5 C-3346 169±11 17±2 >200 458±6 C-3350 16±5 49±5 136±6 80±8 C-3353 31±1 >500 92±8 53±9 C-3355 20±1 39±1 247±14 276±9 C-3357 30±1 61±3 25±6 295±9 C-3362 32±5 25±6 19.1±1 40±9 C-3364 29±4 11±3 21±0.3 22±2 C-3365 28±4 21±4 4.6±0.1 7.3±0.5 C-3366 11±2 11±2 20±0.2 9.1±0.6 C-3368 28±1 28±5 26±3 16±4 C-3369 10±2 22±1 22±2 21±1 C-3371 15±3 25±1 36±7 11±1 C-3373 4.8±0.8 43±6 19±1 19±2 C-3374 4.6±0.3 25±5 6.7±0.2 4.9±0.6 C-3375 22±4 55±5 75±4 12±2 C-3376 1.3±0.1 11±1 2.3±0.2 27±2 C-3377 6.1±0.3 16±1 7.8±1.4 4.8±0.1 C-3380 28±4 157±25 32±7 44±10 C-3383 12±1 50±7 7.3±0.5 80±6 C-3384 14±3 56±6 5.5±0.6 40±5 C-3385 8.0±0.7 20±2 7.0±0.7 16±3 C-3389 36±3 49±2 32±3 47±6 C-3390 7.9±0.9 11±2 18±0.1 20±0.3 C-3391 7.8±1.0 38±4 20±0.3 22±2 C-3393 0.46±0.04 35±1 32±4 29±3 C-3397 9.3±1.7 36±5 38±2 62±4 C-3398 7.4±0.8 34±6 17±3 23±3 C-3399 7.9±0.7 55±7 17±1 41±6 C-3400 11±1 24±2 24±5 33±1 C-3402 4.6±0.1 14±2 39±5 43±8 C-3403 6.7±0.9 38±5 16±1 11±3 C-3427 5.9±0.5 20±5 9.3±1 13±2 C-3459 >500 n.e. n.e. n.e. C-3511 n.t. 61±4 5.4±0.3 28±3 C-3517 n.t. 74±4 12±1 18±1 C-3520 n.t. 45±6 16±2 30±1 C-3532 74±1 181±33 27±2 103±2 C-3535 84±3 35±7 107±11 81±0 C-3537 17±1 27±2 28±3 35±1 C-3539 20±1 23±1 40±5 113±6 C-3546 0.13±0.02 73±10 14±1 32±7 C-3548 9.2±1.0 45±13 57±9 37±3 C-3559 372±23 260±55 128±8 154±25 C-3562 31±2 36±6 24±2 57±5 C-3570 12±1 13±1 14±3 29±2 C-3591 9.9±0.9 27±4 12±3 16±2 C-3593 16±1 25±4 20±1 9±2 C-3594 15±1 7.2±0.6 6.1±2.4 10±2

Example 4. Antiproliferative Effect of PDIAl-inhibitors in Vitro in Hypoxic Conditions and in Cancer Cells Stimulated with Estrogen

[0088] Anticancer activity of PDI A1-inhibitors has been also tested in vitro in antiproliferative essay in normoxic and hypoxic conditions as well in estrogen-stimulated cancer cells. In the experiment, cells were seeded on 96-well plates (Sarstedt, Germany) in appropriate culture medium at a density of 10.sup.5 cells/mL 24 h before adding the tested compounds. Cells were treated with each compound in four concentrations in the range 0.1-100 ug/mL. Cisplatin (Ebewe, Austria) in the range 0.01 -10 ug/mL was used as a reference drug. Dimethyl sulfoxide (DMSO), used as a stock solution solvent, was tested for antiproliferative activity and it did not affect cell proliferation at 0.1% (v/v) - a highest concentration used in compound solutions. After 72 h of compound treatment at 37° C., 5 % CO.sub.2 humid atmosphere and in wo different oxygen level conditions: 21% - normal and <1% - hypoxia. In some experiments, the MDA-MB-231 and MCF-7 cells were seeded with or without 200 nM estradiol and after 24 h the tested compounds were added. A previously described sulforhodamine B antiproliferative assay was used with minor modifications (Skehan P et al., 1990). Briefly, cells were fixed with 50 .Math.L/well of 50% (w/v) trichloroacetic acid (Avantor Performance Materials, Gliwice, Poland). After 1 h incubation, plates were washed several times with tap water and 50 .Math.L of 0.4% (w/v) solution of sulforhodamine B (Sigma-Aldrich, Germany) in 1% (v/v) acetic acid (Avantor Performance Materials, Gliwice, Poland) was added to each well. After 30 min incubation at room temperature, unbound dye was washed out with 1% (v/v) acetic acid, whereas bound dye was solubilized with 10 mM unbuffered TRIS (Avantor Performance Materials, Gliwice, Poland) solution. The entire procedure was performed using a BioTek EL-406 washing station (BioTek Instruments, USA). After additional 30 min, absorbance was read using a Biotek Hybrid H4 reader (BioTek Instruments, USA) at 540 nm wavelength. MTT assay was used alternatively for HL-60 cell line and in the experiment in which estrogens are added (specified in the table legend). Absorbance was measured using a Biotek Hybrid H4 reader at 570 nm wavelength for MTT assay.

[0089] Compounds at each concentration were tested in triplicate in a single experiment and each experiment was repeated at least three times independently.

[0090] Results of in vitro antiproliferative effects are shown in Table 3 and Table 4 and are presented as mean IC.sub.50 ± SD calculated using the Prolab-3 system based on Cheburator 0.4 software.

TABLE-US-00004 Antiproliferative effect of PDI A1inhibitors in normal (21% of oxygen) and hypoxia (<1% of oxygen) conditions against human cancer cell lines (72- hour exposition). Compd Cell line/condition IC50 [.Math.g/ml] MCF-7 MDA-MB-231 Caco-2 HT-29 normal hypoxia normal hypoxia normal normal C-3161 3.6 ± 0.3 3.6 ± 0.3 9.9 ± 8.2 11.3 ± 10.6 3.5 ± 0.3 28.38 ± 5.0 C-3251 8.8. ± 8.2 7.9 ± 6.5 24.0 ± 6.4 26.5 ± 1.3 3.4 ± 0.2 30.2 ± 4.7 C-3257 20.8 ± 6.6 17.1 ± 7.4 9.9 ± 2.8 13.5 ± 4.0 9.8 ± 3.8 23.8 ± 4.8 CCF642 0.7± 0.5 0.6 ± 0.6 0.3 ± 0.1 0.3 ± 0.2 0.4 ± 0.1 0.4 ± 0.05 LOC14 4.4 ± 0.9 3.9 ± 0.3 2.8 ± 0.4 2.6 ± 0.5 9.1 ± 3.4 12.6 ± 8.4 Cisplatin 1.8 ± 0.3 1.3 ± 0.5 3.2 ± 0.5 3.1 ± 0.9 2.3 ± 0.5 2.82 ± 0.6

TABLE-US-00005 The antiproliferative effect of PDI A1inhibitors towards human breast cancer cell lines pretreated or not with estradiol and for comparison towards human colon cancer and leukemia cellline line (72 hours exposition). Cmpd Cell line/condition IC50 [.Math.g/ml] Selectivity index (SI): IC50 of MCF-10A/ IC50 of MCF-7 MDA-MB-231 MCF-7 HT-29 HL-60 normal + estradiol normal + estradiol normal normal C-3380 26.1 ± 1.0 26.3 ± 2.5 25.5 ± 2.3 26.3 ± 4.3 34.6 ± 2.2 5.3 ± 2.8 0.75 C-3389 23.2 ± 1.0 28.0 ± 1.7* 26.7 ± 4.5 18.4 ± 4.3 31.2 ± 6.7 2.8 ± 0.8 0.23 C-3353 24.2 ± 2.6 25.7 ± 1.9 6.2 ± 1.8 5.8 ± 1.3 35.9 ± 1.3 2.0 ± 0.1 3.36 C-3287 6.4 ± 0.8 23.8 ± 2.3* 31.3 ± 0.6 29.3 ± 4.1 31.5 ± 4.9 0.5 ± 0.3 1.10 C-3326 15.7 ± 3.1 17.7 ± 2.1 5.4 ± 1.7 10.4 ± 2.4 39.2 ± 6.5 1.9 ± 0.6 4.84 C-3251 26.6 ± 2.3 29.7 ± 1.9 3.9 ± 0.5 4.0 ± 0.2 37.2 ± 8.4 1.5 ± 0.1 6.62

Statistical analysis: Unpaired t test. *p<0.05 as compared to appropriate cells not pretreated with estradiol. MTT assay was used for antiproliferative activity assessment.

[0091] In reference to Table 3 and Table 4, among all PDI A1inhibitors tested in normal condition, the most active towards all cell lines were C-3161 and C-3251. The activity of these compounds was comparable to reference LOC14. In reference to Table 3, the antiproliferative effect of several PDIA1 inhibitors was compared at different oxygen supplies, which showed that their antiproliferative effect on human breast cancer cells MCF-7 and MDA-MB-231 is not dependent on oxygen access. Therefore, it seems that these compounds may also be active in the hypoxic environment of the tumor. In reference to Table 4, a slight decrease of antiproliferative activity towards MDA-MB-231 cell line of PDI A1 inhibitors C-3389 and C-3287 has been demonstrated during simultaneous incubation with estradiol. For the MCF-7 cell line, a slight decrease in sensitivity after addition of estradiol was observed with the inhibitor C-3326. These results suggest modulation of PDIA1 expression in cancer cells by estradiol.

Example 5. The Influence of PDI A1inhibitors on the Clonogenic Potential, Cell Cycle and Cell Death of Human Colon Cancer Cell Lines

[0092] To confirm, anticancer effects, selected compounds of invention, PDIA1 inhibitors were tested in long-term colony formation assay. For long-term colony formation assay the human colorectal carcinoma cell lines Caco-2 and HT-29 were maintained as follows: HT-29 in RPMI-1640 with HEPES + OPTI-MEM (1:1) and Caco-2 in Eagle’s medium (all from IIET, Wroclaw, Poland) both culture media were supplemented with 2 mM L-glutamine, 1 mM sodium pyruvate (both from Sigma-Aldrich Chemie GmbH, Steinheim, Germany), fetal bovine serum: 5% HT-29 (GE Healthcare), 20% Caco-2 (Sigma-Aldrich Chemie GmbH, Steinheim, Germany), 100 U/ml penicillin, 100 .Math.g/ml streptomycin (both from Polfa Tarchomin S.A., Warsaw, Poland). All cell lines were grown at 37° C. in a humidified atmosphere with 5% CO.sub.2. 24 h before adding the tested compounds, cells were seeded on 24-well plates (Corning, Germany) in appropriate culture medium (described for each cell line in details below) at a density of 1.5× 10.sup.5 cells/mL. The cells were treated with tested compounds in the doses of IC50 for each compound and collected after three more days. The viable cells were counted using a hemocytometer (trypan blue exclusion method) and seeded in triplicates at a density of 5 × 10.sup.2 cells/3 ml and 2.5 × 10.sup.2 cells/3 ml (9.5 cm.sup.2) for Caco-2 and HT-29 respectively. The dishes had been pre-coated with poly-L-lysine/PBS (0.001%; Sigma-Aldrich) and washed twice with PBS (with Ca.sup.2+ and Mg.sup.2+). After 2 weeks, the colonies were fixed and stained with 1% crystal violet/ethanol (Sigma-Aldrich), documented with Sony Alpha 300 camera (Sony), and counted manually using ImageJ 1.47 software (National Institutes of Health, Bethesda, MD, USA). Surviving fraction (SF) was calculated. The concentrations of disclosed compounds were chosen on the basis of IC50 values CCF642: 0.4 .Math.g/ml, LOC14: 10 .Math.g/ml on both cell lines; C-3251: 30 .Math.g/ml on HT-29 and 3 .Math.g/ml on Caco-2.

[0093] In reference to FIGS. 1A and 1B, the ability of C-3251 (as the representative for PDI A1 inhibitors) to inhibit long-term colonies formation was much potent towards HT-29 than CaCo-2 cell line, opposite to the results of proliferation inhibition test. Reference compounds inhibit colonies formation only of Caco-2 cell line (FIGS. 1A and 1B). FIG. 1B shows representative plates with the use of disclosed compounds from clonogenic assay.

[0094] Cell cycle and cell death analysis has been performed as previously described (Milczarek M et al. , 2015). Compounds were tested 5 times independently. Obtained results were analyzed using BD FACSDiva 6.2 software. In reference to FIG. 1C, C-3251 increased the percentage of CaCo-2 cells in S cell cycle phase. This compound decreased HT-29 cells in G0/G1 and increased in G2/M phase. In reference to FIG. 1D, C-3251 also increased significantly the percentage of death HT-29 cells.

[0095] Caspase-3/7 activity assay has been performed as previously described (Milczarek M et al., 2015) after 24 and 48 h of incubation with disclosed compounds. Compounds were tested in triplicate in a single experiment and each experiment was repeated three times independently. Results were normalized to the protein content using the SRB method and reported as mean relative caspase-3/7 activity compared to the control sample ± SD.

[0096] In reference to FIG. 1E and FIG. 1F, caspase 3/7 induction was higher on HT-29 cell line after incubation with all compounds as compare to Caco-2 cell line. C-3251 significantly increase caspase 3/7 activity towards Caco-2 cells after 48 h treatment and towards HT-29 cells after 24 and 48 h of incubation. Dashed line designated control level. Statistical analysis: Dunn’s or Dunett’s multiple comparison tests. *p<0.05 as compared to control.7

Example 6. Evaluation of Effects of PDI A1inhibitors on Transendothelial Cancer Cells Migration in in Vitro Model

[0097] To assess whether compounds of invention, PDI A1-inhibitors are also effective as inhibitors of cancer cell transmigration through endothelium the transmigration assay with MDA-MB-231/lung microvascular endothelium was used as described previously (Stojak et al., 2018). Cell migration was assayed in 24-well, 6.5-mm internal-diameter Transwell plates (8.0 .Math.M pore size; BD Pharmingen). Human lung microvascular endothelial cells (hLMVECs) were seeded into 24-well plates (seeding density 5 × 10.sup.4 cells/insert) on the upper side of the filter and left to grow to confluence. After confluent monolayer formation, hLMVECs were pre-treated with 10 ng/mL IL-1β for 6 h. Prior to use in transmigration assay, cancer cells were pre-incubated with various concentrations (3, 10, 30, 50, 100 .Math.M) of tested inhibitors of PDIA1, C-3380, C-3389 for 30 min. Then, MDA-MB-231 cells (each 5×10.sup.4 per well) were placed into upper chambers and tested PDI A1inhibitors (see above) or bepristat, a reference pharmacological inhibitor of PDIA1, at various concentrations (1, 10, 30, 50, 100 .Math.M were given. Lower chambers were filled with medium containing chemoattractant (20% FBS or 100 ng/mL SDF-1α). After 24 h of co-culture, hLMVEC monolayers and non-migrating cancer cells on the upper surface of the membrane were removed. Migrated cancer cells on the undersides of the Transwell membranes were detached and stained by Calcein-AM-Accutase solution for 60 minutes. The cell number was determined by measuring the fluorescence using plate reader. Experiments were performed in triplicates and repeated three times.

[0098] In reference to FIG. 2A, it is shown the influence of bepristat 2a and C-3380 on MDA-MB-231 cell transmigration across IL-1β 10 ng/mL (6 hours) - stimulated hLMVECs. The number of migrating MDA-MB-231 cells through the hLMVEC monolayer was quantified by measuring the fluorescence, as described in Methodology. Data represent mean ± SD of three independent experiments. Statistical analysis was performed using one-way ANOVA. Symbols mark the statistical significance levels as follows: (*) indicates p<0.05 as compared to IL-1β 10 ng/mL stimulated group.

[0099] In reference to FIG. 2B, it is shown the influence of bepristat and C-3389 on MDA-MB-231 cell transmigration across IL-1β 10 ng/mL (6 hours) - stimulated hLMVECs. The number of migrating MDA-MB-231 cells through the hLMVEC monolayer was quantified by measuring the fluorescence, as described in Methodology. Data represent mean ± SD of three independent experiments. Statistical analysis was performed using one-way ANOVA. Symbols mark the statistical significance levels as follows: (*) indicates p<0.05 as compared to IL-1β 10 ng/mL stimulated group.

[0100] Tested compounds inhibited transmigration of breast cancer cells across hLMVEC monolayer in a concentration -dependent manner.

Example 7. Anticancer Effects of PDI Al-inhibitors in Vivo

[0101] To confirm anticancer activity of selected compounds of invention, PDI A1-inhibitors in vivo, selected compounds of invention were tested in the murine model of Lewis Lung Carcinoma (LLC). The Lewis Lung Carcinoma (LLC) cell line was obtained from the ATCC collection and was cultured in a humidified atmosphere of 5% CO.sub.2 at 37° using Dulbecco’s modified Eagle’s medium (DMEM) that contained 10% bovine serum (Sigma). Female (6-8 weeks old) C57BL/6 mice (purchased from Envigo RMS. BV., Nederland) were acclimated for one week and were fed with animal chow and water ad libitum. The C57BL/6 mice were injected s.c. with 0.5 × 10.sup.5 LLC cells per mice in 100 .Math.L PBS. Compounds were dissolved in DMSO and then 0.9% NaCl (DMSO final concentration 1%) were added. In each treatment group, i.p. injections of 100 .Math.l compound were started on 1 day after tumor inoculation. Control animals injected with equal volume of 0.9% NaCl with 1% DMSO administered in the same schedule as other groups. Tumor larger radius (a) and smaller radius (b) were measured by calipers. The tumor volume (Tv) was calculated according the following formulaTv = V=4 • ab2/3. The mice in control group were sacrificed 17 days after tumor establishment. Tumor tissues were dissected, weighed and frozen in OCT compound.

TABLE-US-00006 The individual tumor volumes (mm3) of mice in group treated with C-3161 and control group Nr.of animal treated with C-3161 (50 mg/kg) Day of experiment 10 12 14 16 17 1 258 496 829 980 946 2 0 0 254 199 476 3 0 0 0 0 0 4 0 0 0 0 0 5 266 365 642 719 419 average±stdev 105±144 172±240 345±377 380±446 368±393 Nr.of animal (control group) 1 0 617 875 1206 1255 2 201 305 435 576 548 3 151 389 1110 1338 1354 4 0 429 1119 1182 1176 5 60 412 979 1486 1714 average±stdev 82±91 430±115 904±281 1158±347 1209±423 TTEST.sup.a 0.78 0.06 0.03 0.02 0.01

TABLE-US-00007 The individual tumor volumes (mm3) of mice in group C-3257 and control group Nr.of animal treated with C-3257 (75 mg/kg) Day of experiment 10 12 14 16 17 1 0 572 594 794 674 2 0 0 0 548 882 3 329 468 537 601 1016 4 0 0 657 772 1016 5 0 0 523 717 986 average±stdev 66±147 208±287 462±264 686±108 1097±482 Nr.of animal (control group) 1 0 617 875 1206 1255 2 201 305 435 576 548 3 151 389 1110 1338 1354 4 0 429 1119 1182 1176 5 60 412 979 1486 1714 average±stdev 82±91 430±115 904±281 1158±347 1209±423 TTEST.sup.a 0.36 0.25 0.13 0.04 0.03

In reference to Tables 6,and 7, it was established that compounds of invention: C-3161, C-3257 possess anti-cancer activity in vivo. Results of anticancer activities of C-3161, C-3257 are also shown in FIG. 4.

[0102] In reference to FIG. 5, anti-cancer effects were also shown for the compounds C-3281 and C-3329. These compounds diminished tumour volume but did not modified animal weight suggesting that they display clear-cut anticancer activity in vivo, without evident toxicity as evidenced by lack of the effects on the animal weight.

Example 8. Evaluation of Anti-thrombotic Effects of PDIA1 Inhibitors in Vivo

[0103] To confirm antithrombotic activity of compounds of invention, inhibitors of PDIA1, pharmacological activity of selected compounds was tested in vivo in the rat model of arterial thrombosis . Wistar rats were anaesthetized with pentobarbital (40 mg/kg, i.p.) and placed in a supine position on a heated (37° C.) operating table. Arterial thrombosis was induced by electrical stimulation of the right common carotid artery, as previously described (Kramkowski et al., 2012). Briefly, the anode, a stainless steel L-shaped wire, was inserted under the artery and connected to a constant current generator. The cathode was attached subcutaneously to the hind limb. The artery was stimulated (1 mA) for 10 min. Fifty-five minutes after the beginning of stimulation, the segment of the common carotid artery containing the formed thrombus was dissected and opened lengthwise, and the thrombus was completely removed and air-dried at room temperature for 24 h. Thrombus was then weighed in a blinded manner. As shown in FIG. 5, reference PDI inhibitors rutin inhibited thrombus formation in vivo in the rat model of arterial thrombosis while isoquercetin was less effective. FIG. 5 also shows anti-thrombotic effects of

[0104] C3989 and C-3257 two among compounds of invention in in vivo rat model of arterial thrombosis. FIG. 6 shows dose-dependent effects induced by C-3257 on thrombus formation in in vivo rat model of arterial thrombosis. As can be noted in FIG. 6 effects of C-3257 on thrombus formation in vivo was significant and pronounced at a dose as low as 0.03 .Math.mol/kg.

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