Bioorganic & Medicinal Chemistry 2013-04-01

Novel leucine ureido derivatives as inhibitors of aminopeptidase N (APN).

Chunhua Ma, Kang Jin, Jiangying Cao, Lei Zhang, Xiaoguang Li, Wenfang Xu

Index: Bioorg. Med. Chem. 21(7) , 1621-7, (2013)

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Abstract

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 leucine ureido derivatives as aminopeptidase N (APN/CD13) inhibitors. The results showed that compound 8c had the most potent inhibitory activity against APN with the IC50 value to 0.06 ± 0.041 μM, which could be used for further anticancer agent research.Copyright © 2013 Elsevier Ltd. All rights reserved.