Novel aminopeptidase N (APN/CD13) inhibitors derived from 3-phenylalanyl-N′-substituted-2,6-piperidinedione

Aminopeptidase N (APN/CD13) over expressed on tumor cells, plays a critical role in tumor invasion, metastasis, and tumor angiogenesis. Here we described the design, synthesis and preliminary activity studies of novel APN inhibitors with 3-phenylalanyl-N′-substituted-2,6-piperidinedione scaffold. The results showed that compound 7c had the most potent inhibitory activity against APN with the IC50 value to 5.00 ± 3.17 μM, which could be used as the lead compound in the future for anticancer agent research.

A series of novel 3-phenylalanyl-N′-substituted-2,6-piperidinedione derivatives were synthesized and evaluated for their in vitro enzymatic inhibitory activities against aminopeptidase N. Compound 7c had the most potent inhibitory activity against APN with the IC50 of 5.00 ± 3.17 μM.Figure optionsDownload as PowerPoint slide