Novel 3-phenylpropane-1,2-diamine derivates as inhibitors of aminopeptidase N (APN).
Novel 3-phenylpropane-1,2-diamine derivates as inhibitors of aminopeptidase N (APN).
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DOI：
10.1016/j.bmc.2008.10.025
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发表时间：
2008-12
影响因子：
3.5
通讯作者：
Luqing Shang;Qiang Wang;H. Fang;J. Mu;Xuejian Wang;Yumei Yuan;B. Wang;Wenfang Xu
中科院分区：
文献类型：
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作者：
Luqing Shang;Qiang Wang;H. Fang;J. Mu;Xuejian Wang;Yumei Yuan;B. Wang;Wenfang Xu
氨肽酶N（APN）是参与肿瘤侵袭和转移过程的必需肽酶。在这里，我们描述了一类新型抑制剂，以 3-苯基丙烷-1,2-二胺作为 APN 的支架。酶抑制研究的初步活性评估表明，化合物12i对APN表现出强效、选择性的抑制活性，IC50值为15.5±1.2μM。
Aminopeptidase N (APN) is an essential peptidase involved in the process of tumor invasion and metastasis. Here we describe a novel class of inhibitor with 3-phenylpropane-1,2-diamine as scaffold to APN. Preliminary activity evaluation with enzyme inhibition studies showed that compound 12i exhibited potent and selective inhibitory activity towards APN with the IC50value 15.5±1.2μM.