MMPs inhibitors: new succinylhydroxamates with selective inhibition of MMP-2 over MMP-3

Bioorg Med Chem Lett. 2003 Sep 1;13(17):2843-6. doi: 10.1016/s0960-894x(03)00590-0.

Abstract

Some ilomastat analogues featuring an isobutylidene group or a 2-substituted indole nucleus were synthesized to evaluate their inhibitory activities against gelatinase A and stromelysin-1. Potent MMP-2 inhibition and good selectivity for that enzyme have been observed for compounds 1a, 2 and 22.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Hydroxamic Acids / chemical synthesis
  • Hydroxamic Acids / chemistry*
  • Hydroxamic Acids / pharmacology*
  • Indoles / chemistry
  • Indoles / pharmacology
  • Inhibitory Concentration 50
  • Matrix Metalloproteinase Inhibitors*
  • Protease Inhibitors / chemical synthesis
  • Protease Inhibitors / chemistry*
  • Protease Inhibitors / pharmacology*
  • Recombinant Proteins / antagonists & inhibitors
  • Structure-Activity Relationship

Substances

  • Hydroxamic Acids
  • Indoles
  • Matrix Metalloproteinase Inhibitors
  • Protease Inhibitors
  • Recombinant Proteins
  • ilomastat