Novel leucine ureido derivatives as aminopeptidase N inhibitors. Design, synthesis and activity evaluation
Novel leucine ureido derivatives as aminopeptidase N inhibitors. Design, synthesis and activity evaluation
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作为氨肽酶 N 抑制剂的新型亮氨酸脲基衍生物。
DOI：
10.1016/j.ejmech.2015.11.021
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发表时间：
2016-01-27
影响因子：
6.7
通讯作者：
Zhang, Yingjie
中科院分区：
文献类型：
--
作者：
Ma, Chunhua;Cao, Jiangying;Zhang, Yingjie
氨基肽酶N(APN/CD13)在肿瘤细胞和肿瘤微环境中过表达，在肿瘤的侵袭、转移和血管生成中起重要作用。本文介绍了新型氨基肽酶N(APN/CD13)抑制剂亮氨酸脲衍生物的设计、合成及初步活性研究。结果表明，化合物7a对APN的抑制活性最强，其ICso值为20 nM，可用于抗癌药物的进一步研究。(C)2015年爱思唯尔·马森公司。版权所有。
Aminopeptidase N (APN/CD13) over -expressed on tumor cells and tumor microenvironment, plays critical roles in tumor invasion, metastasis and 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 7a had the most potent inhibitory activity against APN with the ICso value of 20 nM, which could be used for further anticancer agent research. (C) 2015 Elsevier Masson SAS. All rights reserved.