Discovery of New 4-Alkoxyquinazoline-Based Derivatives as Potent VEGFR2 Inhibitors
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.
4-alkoxyquinazoline-bascd derivatives molecular docking VEGFR2 inhibitors
Yong Yin Shao Sha Yan-Ting Wang Xun Wu She-Feng Wang Fang Qiao Peng-Cheng Lv Hai-Liang Zhu
State Key Laboratory of Pharmaceutical Biotechnology,Nanjing University,Nanjing 210093,China
国内会议
大连
英文
332-338
2016-09-24（万方平台首次上网日期，不代表论文的发表时间）