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KMID : 0043320080310101231
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Archives of Pharmacal Research
2008 Volume.31 No. 10 p.1231 ~ p.1239
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The Synthesis and Preliminary Activity Assay In Vitro of Peptide-like Derivatives as APN Inhibitors
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Liu Cheng-Mei
Tu Guo-Gang
Xiong Fang
Huang Hui-Ming
Li Shao-Hua
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Abstract
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Both the aminopeptidase N (APN) and matrix metalloproteinase (MMP) are essential metallopeptidases in the development of tumor invasion and angiogenesis. A series of novel peptide-like derivatives were designed and synthesized as antitumor agents. Their structures were confirmed by IR, MS, and 1H-NMR. These compounds exhibited potent inhibitory activities against APN and low activity against MMP in vitro. The derivatives with methoxy group show better activities than those with other substituted group and could be used as lead compounds for exploring new APN inhibitors in the future.
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KEYWORD
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Synthesis, APN inhibitor, Antitumor activity
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