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

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 IC50 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.

A series of novel quinoxalinone peptidomimetic derivatives (A1–A19) were synthesized and evaluated for their in vitro enzymatic inhibitory activities against aminopeptidase N (APN/CD13) and MMP-2.Figure optionsDownload as PowerPoint slide