Discovery of New 4-Alkoxyquinazoline-Based Derivatives as Potent VEGFR2 Inhibitors

来源 :第八届国际分子模拟与信息技术应用学术会议 | 被引量 : 0次 | 上传用户：tianhaiyandml

【摘要】

：

　　VEGFR2 has been proved to play a major role in the regulation of tumor angiogenesis.Twenty-one 4-alkoxyquinazoline-based derivatives have been designed and

【作者】

：

YongYin;ShaoSha;Yan-TingWang;XunWu;She-FengWang;FangQiao;Peng-ChengLv;Hai-LiangZhu;

【机构】

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State Key Laboratory of Pharmaceutical Biotechnology,Nanjing University,Nanjing 210093,China

【出处】

：

第八届国际分子模拟与信息技术应用学术会议

【发表日期】

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2016年期

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　　VEGFR2 has been proved to play a major role in the regulation of tumor angiogenesis.Twenty-one 4-alkoxyquinazoline-based derivatives have been designed and synthesized as vascular endothelial growth factor receptor 2(VEGFR2)inhibitors,and their biological activities were evaluated.Among these compounds,compound 3h exhibited the most potent inhibitory activities against VEGFR2 tyrosine kinase and cell proliferation,with the IC50 values of 2.89 nw(for VEGFR2)and 0.25 μM(for MCF-7),which were comparable with the control compound.Docking simulation was performed to position compound 3h into the 4ASE active site,and the result showed that compound 3h could bind well at the 4ASE active site.

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Discovery of New 4-Alkoxyquinazoline-Based Derivatives as Potent VEGFR2 Inhibitors

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