Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594173 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
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 80Â 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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Authors
Eric Turtle, Nicholas Chow, Charles Yang, Sergio Sosa, Udo Bauer, Mitch Brenner, David Solow-Cordero, Wen-Bin Ho,