Synthesis, Molecular Modeling and Biological Evaluation of 4-Alkoxyquinazoline Derivatives as Novel Inhibitors of VEGFR2

Liang Lu; Ting-Ting Zhao; Tian-Bao Liu; Wen-Xue Sun; Chen Xu; Dong-Dong Li; Hai-Liang Zhu

doi:10.1248/cpb.c16-00386

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Synthesis, Molecular Modeling and Biological Evaluation of 4-Alkoxyquinazoline Derivatives as Novel Inhibitors of VEGFR2

Liang Lu, Ting-Ting Zhao, Tian-Bao Liu, Wen-Xue Sun, Chen Xu, Dong-Dong Li, Hai-Liang Zhu

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Keywords: quinazoline, Schiff’s base, vascular endothelial growth factor receptor 2, anticancer

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Supplementary material

2016 Volume 64 Issue 11 Pages 1570-1575

DOI https://doi.org/10.1248/cpb.c16-00386

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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=0.15 µg/mL for A549 and IC₅₀=0.24 µg/mL for MCF-7). Docking simulation had been performed to position compound 4t into the vascular endothelial growth factor receptor (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.

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