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.
Yonggang Li  1 ,  Jian Zhang ,  Wenfang Xu ,  Huawei Zhu ,  Xun Li
Affiliations
  • 1. School of Pharmaceutical Sciences, Shandong University, Ji'nan, 250012 Shandong Province, PR China.
PMID: 20097082 DOI: 10.1016/j.bmc.2010.01.008
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.