Synthesis,molecular modeling and biological evaluation of 4-alkoxyquinazoline derivatives as novel inhibitors of VEGFR2
A series of novel quinazoline derivatives have been designed and synthesized,and their inhibitory activities have also been tested against A549(carcinomic human alveolar basal epithelial cell),MCF-7(breast cancer)and Hela(cervical cancer cell).Of these compounds,compound 4t showed the most potent inhibitory activity(IC50= 0.22 μg/mL for Hela,IC50= 0.15μg/mL for A549 and IC50 = 0.24μg/mL for MCF-7).Docking simulation had been performed to position compound 4t into the VEGFR active site to determine the probable binding model.These results suggested that compound 4t with potent inhibitory activity in tumor growth inhibition may be a potential anticancer agent.
Quinazoline Schiff”s base VEGFR2 Anticancer
Liang Lu Ting-Ting Zhao Tian-Bao Liu Wen-Xue Sun Chen Xu Dong-Dong Li Hai-Liang Zhu
State Key Laboratory of Pharmaceutical Biotechnology,Nanjing University,Nanjing 210093,People”s Repu College of Chemical Engineering,Nanjing Forestry University,Nanjing 210073,People”s Republic of Chin
国内会议
大连
英文
927-945
2016-09-24（万方平台首次上网日期，不代表论文的发表时间）