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Design, synthesis and biological evaluation of novel 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as aminopeptidase N/CD13 inhibitors.

Research paper by Xiaopan X Zhang, Jian J Zhang, Lei L Zhang, Jinghong J Feng, Yingying Y Xu, Yumei Y Yuan, Hao H Fang, Wenfang W Xu

Indexed on: 14 Sep '11Published on: 14 Sep '11Published in: Bioorganic & Medicinal Chemistry



Abstract

A series of novel 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives were designed, synthesized and assayed for their activities against aminopeptidase N (APN/CD13) and MMP-2. The results showed that most compounds exhibited higher inhibitory activities against APN than that of MMP-2. Within this series, compound 12h (IC(50)=6.28 ± 0.11 μM) showed similar inhibitory activities compared with Bestatin (IC(50)=5.55 ± 0.01 μM), and it could be used as novel lead compound for the future APN inhibitors development as anticancer agents.