Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363

This article has now been updated. Please use the final version.

Synthesis, molecular modeling and biological evaluation of 4-alkoxyquinazoline derivatives as novel inhibitors of VEGFR2
Liang LuTing-Ting ZhaoTian-Bao LiuWen-Xue SunChen XuDong-Dong Li Hai-Liang Zhu
Author information
JOURNAL FREE ACCESS Advance online publication

Article ID: c16-00386

Details
Abstract

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 = 0.24 μg/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.

Content from these authors
© 2016 The Pharmaceutical Society of Japan
feedback
Top