Novel 3-galloylamido-N′-substituted-2,6-piperidinedione-N-acetamide peptidomimeties as metalloproteinase inhibitors
Novel 3-galloylamido-N′-substituted-2,6-piperidinedione-N-acetamide peptidomimeties as metalloproteinase inhibitors
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DOI：
10.1016/j.bmcl.2006.12.095
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发表时间：
2007-05-15
影响因子：
2.7
通讯作者：
Xu, Wenfang
中科院分区：
文献类型：
--
作者：
Li, Qianbin;Fang, Hao;Xu, Wenfang
Both of aminopeptidase N (APN) and matrix metalloproteinase (MMP) are essential metallopeptidases in the development of tumor invasion and angiogenesis. Novel potent peptidomimetic inhibitors, containing 3-galloylamido-N'-substituted-2, 6-piperidinedione-N-acetamide, have been designed and synthesized according to the conformational constraint strategy. The preliminary biological test showed that most of the compounds displayed high inhibitory activity against MMP-2 and low activity against APN except compounds 6 (IC50 = 3.1 mu M) and 41 (IC50 = 5.2 mu M) which exhibit similar potency to Bestatin (IC50 = 2.4 mu M). (c) 2007 Elsevier Ltd. All rights reserved.
