Synthesis and biological evaluation of 4-(2-fluorophenoxy)-3,3′-bipyridine derivatives as potential c-met inhibitors
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- 作者：Sijia Zhao ; Yu Zhang ; Hongyang Zhou ; Shuancheng Xi ; Bin Zou ; Guanglong Bao ; Limei Wang ; Jiao Wang ; Tianfang Zeng ; Ping Gong ; Xin Zhai ; zhaixin_syphu@126.com" class="auth_mail" title="E-mail the corresponding author
- 关键词：Synthesis ; Bipyridine derivatives ; Aza-aryl formamides ; c-Met ; Cytotoxicity
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：14 September 2016
- 年：2016
- 卷：120
- 期：Complete
- 页码：37-50
- 全文大小：1247 K
文摘
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Twenty-five novel 4-(2-fluorophenoxy)-3, 3′-bipyridine derivatives were designed and synthesized.
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Six series of aza-aryl formamide/amine scaffolds as linker were designed to identify the “five-atom regulation”.
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The cytotoxicity of 26c was more potent against MKN-45 and MDA-MB-231 cell lines than Foretinib.
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Compound 23n displayed preferable activity for c-Met kinase (IC50 = 8.2 nM).