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Bioorg Med Chem. 2013 May 1;21(9):2663-70. doi: 10.1016/j.bmc.2012.06.024. Epub 2012 Jun 19.

Novel indoline-2,3-dione derivatives as inhibitors of aminopeptidase N (APN).

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Department of Medicinal Chemistry, School of Pharmacy, Shandong University, 44, West Culture Road, Jinan, Shandong 250012, China.


Aminopeptidase N (APN/CD13), as a zinc-containing ectoenzyme, plays a critical role in the process of tumor angiogenesis, invasion and metastasis. Through the docking-based virtual screening of chemical databases and the further activity assay, we discovered that compound 10c exhibits potent and selective inhibitory ability towards APN. In addition, a series of indoline-2,3-dione derivates have been designed and synthesized as APN inhibitors. The results of preliminary activity evaluation showed that compound 12a (IC(50) = 0.074 ± 0.0026 μM) exhibited the best inhibitory activity against APN, which could be used for further anticancer agent research.

[Indexed for MEDLINE]

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