Design, synthesis and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives as selective c-Met inhibitors

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• 作者：Xiaoqiang Wang^a ; Nan Jiang^a ; Sijia Zhao ; Shuancheng Xi ; Jiao Wang ; Tongfei Jing ; Wenyu Zhang ; Ming Guo ; Ping Gong ; Xin Zhai ; ^{zhaixin_syphu@126.com}
• 关键词：c-Met ; Antitumor activity ; Synthesis ; Molecular docking ; 6 ; 7-Disubstituted-4-(2-fluorophenoxy)quinolines
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2017
• 出版时间：1 February 2017
• 年：2017
• 卷：25
• 期：3
• 页码：886-896
• 全文大小：1657 K
• 卷排序：25

文摘

Twenty-seven novel 6,7-disubstituted-4-(2-fluorophenoxy)quinoline derivatives were designed and synthesized. 1H-Imidazole-4-carboxamido and (E)-3-hydrosulfonylacrylamido linkers were designed. The configurations of compounds 32–42 were unequivocally confirmed as the E isomer. The compound 16 demonstrated remarkably better biological property and c-Met kinase inhibition than Foretinib. Molecular docking analysis was supplied to guide and explain the observed SARs as well.