[Design, synthesis and activity evaluation of novel matrix metalloproteinases inhibitors based on the structure of enzyme]

Yao Xue Xue Bao. 2007 Dec;42(12):1271-81.
[Article in Chinese]

Abstract

A novel inhibitor series for matrix metalloproteinases (MMPs) were designed and synthesized. Using succinate and malonate as zinc binding groups and long hydrophobic substituents to bind with S1' pockets, the compounds showed micromolar inhibition and selectivity for MMP-2 over others. And we found a better activity compound. It is a chance to find a better precursor of MMP-2 inhibitors with activity and bioavailability by further optimization of compounds.

Publication types

  • English Abstract
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Drug Design*
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Matrix Metalloproteinase Inhibitors*
  • Matrix Metalloproteinases / chemical synthesis*
  • Matrix Metalloproteinases / chemistry
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Matrix Metalloproteinase Inhibitors
  • Matrix Metalloproteinases