Al-Oudat, Buthina A. published the artcileDesign, synthesis and biological evaluation of novel glyoxalase I inhibitors possessing diazenylbenzenesulfonamide moiety as potential anticancer agents, HPLC of Formula: 86-48-6, the publication is Bioorganic & Medicinal Chemistry (2020), 28(16), 115608, database is CAplus and MEDLINE.
The enzyme glyoxalase-I (Glo-I) is an essential therapeutic target in cancer treatment. Significant efforts have been made to discover competitive inhibitors of Glo-I as potential anticancer agents. Herein, the synthesis of a series of diazenylbenzenesulfonamide derivatives 3-R-4-R1-C6H3N=NR2 (R = H, sulfamoyl, carboxy; R1 = H, Me, carboxy, sulfo; R2 = 4-amino-6-hydroxynaphthalen-1-yl, 8-hydroxyquinolin-5-yl, 4-hydroxyphenyl, etc.) and their in vitro evaluation against Glo-I and the resulting structure-activity relationships were reported. Among the compounds tested, compounds 3-R-4-R1-C6H3N=NR2 (R = sulfamoyl, R1 = Me, R2 = 8-hydroxyquinolin-5-yl) and (R = sulfamoyl, R1 = Me, R2 = 3-carboxy-4-hydroxynaphthalen-1-yl) exhibited the highest activity with IC50 1.28μM and 1.13μM, resp. Docking studies to explore the binding mode of the compounds identified the key moieties that may contribute to the observed activities. The active compounds will serve as suitable leads for further chem. optimization.
Bioorganic & Medicinal Chemistry published new progress about 86-48-6. 86-48-6 belongs to alcohols-buliding-blocks, auxiliary class Organic Pigment,Natural product, name is 1-Hydroxy-2-naphthoic acid, and the molecular formula is C11H8O3, HPLC of Formula: 86-48-6.
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