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pubmed-article:20943391pubmed:abstractTextVascular endothelial growth factor receptor-2 (VEGFR-2) plays a crucial role in the process of cancer angiogenesis. A series of quinoline amide derivatives were prepared and found to be good inhibitors of VEGFR-2. The inhibitory activities were investigated against VEGFR-2 kinase and human umbilical vein endothelial cells (HUVEC) in vitro. Compound 6 (5-chloro-2-hydroxy-N-(quinolin-8-yl)benzamide) exhibited the most potent inhibitory activity (IC(50)=3.8 and 5.5 nM for VEGFR-2 kinase and HUVEC, respectively). Docking simulation supported the initial pharmacophoric hypothesis and suggested a common mode of interaction at the ATP-binding site of VEGFR-2, which demonstrates that compound 6 is a potential agent for cancer therapy deserving further researching.lld:pubmed
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pubmed-article:20943391pubmed:authorpubmed-author:ShiLeiLlld:pubmed
pubmed-article:20943391pubmed:authorpubmed-author:YangYingYlld:pubmed
pubmed-article:20943391pubmed:authorpubmed-author:ZhouYangYlld:pubmed
pubmed-article:20943391pubmed:authorpubmed-author:ZhuHai-LiangH...lld:pubmed
pubmed-article:20943391pubmed:authorpubmed-author:LiHuan-QiuHQlld:pubmed
pubmed-article:20943391pubmed:authorpubmed-author:ZhuZhen-WeiZWlld:pubmed
pubmed-article:20943391pubmed:copyrightInfoCopyright © 2010 Elsevier Ltd. All rights reserved.lld:pubmed
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pubmed-article:20943391pubmed:articleTitleDesign, synthesis and biological evaluation of quinoline amide derivatives as novel VEGFR-2 inhibitors.lld:pubmed
pubmed-article:20943391pubmed:affiliationState Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, People's Republic of China.lld:pubmed
pubmed-article:20943391pubmed:publicationTypeJournal Articlelld:pubmed
pubmed-article:20943391pubmed:publicationTypeResearch Support, Non-U.S. Gov'tlld:pubmed
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