Design and synthesis of procollagen C-proteinase inhibitors |
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Authors: | Eric Turtle Nicholas Chow Charles Yang Sergio Sosa Udo Bauer Mitch Brenner David Solow-Cordero Wen-Bin Ho |
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Institution: | FibroGen Inc., 409 Illinois St, SF, CA 94158, USA |
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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 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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