期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 28, 期 4, 页码 717-726出版社
INFORMA HEALTHCARE
DOI: 10.3109/14756366.2012.680062
关键词
Aminopeptidase N; inhibitors; L-isoserine tripeptide derivatives; anticancer agents; synthesis
资金
- National High Technology Research and Development Program of China (863 project) [2007AA02Z314]
- National Natural Foundation Research Grant [90713041]
- National Natural Science Foundation of China [21172134]
Aminopeptidase N (APN/CD13) is one of the essential proteins for tumour invasion, angiogenesis and metastasis as it is over-expressed on the surface of different tumour cells. Based on our previous work that L-isoserine dipeptide derivatives were potent APN inhibitors, we designed and synthesized L-isoserine tripeptide derivatives as APN inhibitors. Among these compounds, one compound 16l (IC50 = 2.51 +/- 0.2 +/- mu M) showed similar inhibitory effect compared with control compound Bestatin (IC50 = 6.25 +/- 0.4 mu M) and it could be used as novel lead compound for the APN inhibitors development as anticancer agents in the future.
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