Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 18, Issue 4, Pages 1516-1525Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.01.008
Keywords
Quinoxalinone derivatives; MMP-2 inhibitors; Peptidomimetic; Anti-tumor
Funding
- Natural Science Foundation of China [30701053]
- Foundation of Ministry of Education of the People's Republic of China [20070422061]
- Natural Science Foundation of Shandong Province [Y2008C01]
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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. (C) 2010 Elsevier Ltd. All rights reserved.
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