Design and synthesis of procollagen C-proteinase inhibitors

…, S Sosa, U Bauer, M Brenner, D Solow-Cordero…

Index: Turtle, Eric; Chow, Nicholas; Yang, Charles; Sosa, Sergio; Bauer, Udo; Brenner, Mitch; Solow-Cordero, David; Ho, Wen-Bin Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 24 p. 7397 - 7401

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Citation Number: 6

Abstract

Non-peptidic inhibitors of procollagen C-proteinase (PCP) were designed from substrate leads. Compounds were optimized for potency and selectivity, with N-substituted aryl sulfonamide hydroxamates having the best combination of these properties. Compounds 89 and 60 have IC50 values of 10 and 80nM, respectively, against PCP; excellent selectivity over MMP's 1, 2, and 9; and activity in cell-based collagen deposition assays.