Novel matrix metalloproteinase inhibitors derived from quinoxalinone scaffold (Part I)

Bioorg Med Chem. 2010 Feb 15;18(4):1516-25. doi: 10.1016/j.bmc.2010.01.008. Epub 2010 Jan 11.

Abstract

A series of quinoxalinone peptidomimetic derivatives was designed, synthesized, and assayed for their inhibitory activities on metalloproteinase-2 (MMP-2) and aminopeptidase N (APN). The results showed that all of these quinoxalinone derivatives displayed highly selective inhibition against MMP-2 as compared with APN, with IC(50) values in the micromole range. Compound A3 showed comparable MMP-2 inhibitory activities than the positive control LY52, which might be used as a potential lead in future research on anticancer agents.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Magnetic Resonance Spectroscopy
  • Matrix Metalloproteinase Inhibitors*
  • Models, Molecular
  • Protease Inhibitors / chemistry
  • Protease Inhibitors / isolation & purification
  • Protease Inhibitors / pharmacology*
  • Quinoxalines / chemistry
  • Quinoxalines / isolation & purification
  • Quinoxalines / pharmacology*
  • Spectrometry, Mass, Electrospray Ionization
  • Structure-Activity Relationship

Substances

  • Matrix Metalloproteinase Inhibitors
  • Protease Inhibitors
  • Quinoxalines