Design and synthesis of procollagen C-proteinase inhibitors.

  title={Design and synthesis of procollagen C-proteinase inhibitors.},
  author={Eric Turtle and Nicholas S C Chow and Charles Yang and Sergio Sosa and Udo A Bauer and Mitch Brenner and David E. Solow-Cordero and W B Ho},
  journal={Bioorganic & medicinal chemistry letters},
  volume={22 24},
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.