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

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

  • Bioorg Med Chem. 2011 Oct 15;19(20):6015-25. doi: 10.1016/j.bmc.2011.08.041.
Xiaopan Zhang 1,  Jian Zhang,  Lei Zhang,  Jinghong Feng,  Yingying Xu,  Yumei Yuan,  Hao Fang,  Wenfang Xu
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, School of Pharmacy, Shan Dong University, 44, West Culture Road, Ji'nan 250012, PR China.
PMID: 21911297 DOI: 10.1016/j.bmc.2011.08.041
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.

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