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

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• 作者：Chunhua Ma ; Kang Jin ; Jiangying Cao ; Lei Zhang ; Xiaoguang Li ; Wenfang Xu ; ^{wfxu@yahoo.cn}
• 关键词：Aminopeptidase N ; Inhibitors ; Leucine ureido derivatives ; Synthesis
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2013
• 出版时间：1 April, 2013
• 年：2013
• 卷：21
• 期：7
• 页码：1621-1627
• 全文大小：1199 K

文摘

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 ¡À 0.041 ¦ÌM, which could be used for further anticancer agent research.