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Published on: March 30, 2022
Novel matrix metalloproteinase inhibitors derived from quinoxalinone scaffold (Part I)
Yonggang Li1, Jian Zhang, Wenfang Xu
1School of Pharmaceutical Sciences, Shandong University, Ji'nan, 250012 Shandong Province, PR China.
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.
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