AI Article Synopsis
- Researchers developed non-peptidic inhibitors for procollagen C-proteinase (PCP) using substrate leads as a foundation.
- The most effective compounds identified were N-substituted aryl sulfonamide hydroxamates, showcasing strong potency and selectivity.
- Specifically, compounds 89 and 60 exhibited impressive IC(50) values of 10 and 80 nM against PCP and demonstrated excellent selectivity over certain matrix metalloproteinases (MMPs) while being effective in cell-based assays for collagen deposition.
Article 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 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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| http://dx.doi.org/10.1016/j.bmcl.2012.10.067 | DOI Listing |
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