Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 20, Issue 12, Pages 3807-3815Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2012.04.035
Keywords
Aminopeptidase N; Inhibitors; Amino acid ureido derivatives; Synthesis; Anti-cancer
Funding
- National Natural Science Foundation Research of China [9071304, 30772654]
- National Science and Technology Major Project [2009-ZX09103-118]
- Natural Science Foundation for Young Scholars of Shandong Province [2006BS03021]
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A series of amino acid ureido derivatives as aminopeptidase N (APN/CD13) inhibitors were synthesized and evaluated for their APN inhibitory activities and anti-cancer effects. The results showed that most of these amino acid ureido derivatives exhibited good inhibition against APN, several of which were better than Bestatin. The most active compound 12j (IC50 = 1.1 mu M, compared with Bestatin IC50 = 8.1 mu M) not only possessed much better APN inhibitory activity and anti-proliferation effect on cancer cells, but also exhibited significant block effect of human cancer cell invasion compared with the positive control, Bestatin. These amino acid ureido derivatives could be possibly developed as new APN inhibitors for cancer chemotherapy in the future. (C) 2012 Elsevier Ltd. All rights reserved.
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