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Bioorg Med Chem. 2009 Jul 1;17(13):4666-73. doi: 10.1016/j.bmc.2009.04.056. Epub 2009 May 3.

Design, synthesis and primary activity evaluation of L-arginine derivatives as amino-peptidase N/CD13 inhibitors.

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  • 1Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Ji'nan, Shandong, PR China.

Abstract

A series of L-arginine derivatives were designed, synthesized and assayed for their activities against amino-peptidase N (APN)/CD13 and metalloproteinase-2 (MMP-2). The results showed that most compounds exhibited high inhibitory activities against APN and low activities against MMP-2. Within this series, two compounds 5q and 5s (IC(50)=5.3 and 5.1 microM) showed similar inhibitory activities compared with bestatin (IC(50)=3.8 microM), which could be used as novel lead compounds for the future APN inhibitors development as anticancer agents.

PMID:
19454370
DOI:
10.1016/j.bmc.2009.04.056
[PubMed - indexed for MEDLINE]
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