Patent classifications
C07C381/00
Trithiocarbonate-containing addition-fragmentation agents
The present disclosure provides addition-fragmentation oligomers of the general formula: The crosslinking oligomers of this disclosure provide stress relief by including labile crosslinks that can cleave and reform during the polymerization process. ##STR00001##
Photo-cleavable surfactants
The present invention provides photo-cleavable anionic surfactants, particularly 4-hexylphenylazosulfonate (Azo) and sodium 4-hexylphenylazosulfonate derivatives, which can be rapidly degraded upon UV irradiation, for top-down and bottom-up proteomics. These surfactants can effectively solubilize proteins and peptide fragments with performance comparable to sodium dodecyl sulfate (SDS) and are compatible with mass spectrometry analysis of the solubilized proteins and peptide fragments. Top-down proteomic studies using the present photo-cleavable anionic surfactants has allowed the detection of 100-fold more unique proteoforms as compared to controls and has enabled the solubilization of membrane proteins for comprehensive characterization of protein post-translational modifications. In addition, the present photo-cleavable anionic surfactants are also suitable for dissolving polypeptides in bottom-up proteomic experiments including extracellular matrix proteomics, and are suitable as a substitute for SDS in gel electrophoresis.
Photo-cleavable surfactants
The present invention provides photo-cleavable anionic surfactants, particularly 4-hexylphenylazosulfonate (Azo) and sodium 4-hexylphenylazosulfonate derivatives, which can be rapidly degraded upon UV irradiation, for top-down and bottom-up proteomics. These surfactants can effectively solubilize proteins and peptide fragments with performance comparable to sodium dodecyl sulfate (SDS) and are compatible with mass spectrometry analysis of the solubilized proteins and peptide fragments. Top-down proteomic studies using the present photo-cleavable anionic surfactants has allowed the detection of 100-fold more unique proteoforms as compared to controls and has enabled the solubilization of membrane proteins for comprehensive characterization of protein post-translational modifications. In addition, the present photo-cleavable anionic surfactants are also suitable for dissolving polypeptides in bottom-up proteomic experiments including extracellular matrix proteomics, and are suitable as a substitute for SDS in gel electrophoresis.
KETONE INHIBITORS OF LYSINE GINGIPAIN
The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.
KETONE INHIBITORS OF LYSINE GINGIPAIN
The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.
WDR5-MYC inhibitors
Substituted N-phenyl sulfonamide compounds inhibit WDR5-MYC interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.
WDR5-MYC inhibitors
Substituted N-phenyl sulfonamide compounds inhibit WDR5-MYC interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.
METHOD FOR PRODUCING ARYL COMPOUND CONTAINING TRITYLSULFANYL GROUP
The present invention provides: a substrate for efficiently synthesizing a tritylsulfanyl group-containing aryl compound; a method for producing an SF.sub.5 group-containing compound using the same; and the like. The present invention is a method for producing a tritylsulfanyl group-containing aryl compound, the method including thiotritylation of a halogenated aryl compound represented by the following general formula (1) [wherein A.sup.1 is an aryl group which may have a substituent or a heteroaryl group which may have a substituent; and X is a halogen atom] using [(triphenylmethyl)sulfanyl]potassium or [(triphenylmethyl)sulfanyl]sodium to produce a tritylsulfanyl group-containing aryl compound represented by the following general formula (2) [wherein A.sup.1 is the same as A.sup.1 in the general formula (1); and Ph is a phenyl group].
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Complexes and Compounds of Mercaptophenols and Curcumin for Therapeutic Applications
Complexes and compounds of phenolic molecules possessing two or more ionizable groups, including curcumin, mercaptophenols, and structurally related derivatives, are disclosed. In certain embodiments, a metal or metalloid or nonmetallic atom is directly bonded to the -carbon of curcumin or exclusively to the sulfur atom of a mercaptophenol, conferring enhanced aqueous solubility and stability under physiological and alkaline conditions. The invention includes compositions, processes for preparation, and therapeutic methods employing such complexes and compounds, which may form pharmaceutically acceptable salts suitable for biomedical applications, including parenteral or systemic administration. The complexes and compounds exhibit antiproliferative, anti-migratory, anti-invasive, and immune-stimulatory activities in cell-based and animal models and are suitable for treatment or management of conditions involving abnormal cell proliferation, pathogenic invasion, or dysregulated immune responses.
Complexes and Compounds of Mercaptophenols and Curcumin for Therapeutic Applications
Complexes and compounds of phenolic molecules possessing two or more ionizable groups, including curcumin, mercaptophenols, and structurally related derivatives, are disclosed. In certain embodiments, a metal or metalloid or nonmetallic atom is directly bonded to the -carbon of curcumin or exclusively to the sulfur atom of a mercaptophenol, conferring enhanced aqueous solubility and stability under physiological and alkaline conditions. The invention includes compositions, processes for preparation, and therapeutic methods employing such complexes and compounds, which may form pharmaceutically acceptable salts suitable for biomedical applications, including parenteral or systemic administration. The complexes and compounds exhibit antiproliferative, anti-migratory, anti-invasive, and immune-stimulatory activities in cell-based and animal models and are suitable for treatment or management of conditions involving abnormal cell proliferation, pathogenic invasion, or dysregulated immune responses.