Design and Synthesis of Procollagen C-Proteinase Inhibitors
Bioorganic & medicinal chemistry letters(2012)
摘要
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 IC(50) values of 10 and 80 nM, respectively, against PCP; excellent selectivity over MMP's 1, 2, and 9; and activity in cell-based collagen deposition assays.
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关键词
Procollagen C-proteinase,Fibrosis,Hydroxamate
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