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

作者:Ma, Chunhua; Jin, Kang; Cao, Jiangying; Zhang, Lei; Li, Xiaoguang; Xu, Wenfang*
来源:Bioorganic & Medicinal Chemistry, 2013, 21(7): 1621-1627.
DOI:10.1016/j.bmc.2013.01.068

摘要

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 mu M, which could be used for further anticancer agent research.