Design, synthesis and biological evaluation of novel amino acid ureido derivatives as aminopeptidase N/CD13 inhibitors

L Su, Y Jia, L Zhang, Y Xu, H Fang, W Xu

Index: Su, Li; Jia, Yuping; Zhang, Lei; Xu, Yingying; Fang, Hao; Xu, Wenfang Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 12 p. 3807 - 3815

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Citation Number: 9

Abstract

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 μM, compared with Bestatin IC50= 8.1 μM) not only possessed much better ...