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

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 (IC50 = 6.28 ± 0.11 μM) showed similar inhibitory activities compared with Bestatin (IC50 = 5.55 ± 0.01 μM), and it could be used as novel lead compound for the future APN inhibitors development as anticancer agents.

Novel 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives were designed and synthesized as APN inhibitors. Compound 12h had the best APN inhibition in vitro with the IC50 value to 6.28 ± 0.11 μM, which is similar with that of Bestatin (IC50 = 5.55 ± 0.01 μM).Figure optionsDownload as PowerPoint slide