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■ Synthesis and Evaluation of Biological Properties of 2-(2-(Phenoxy)pyridin-3-yl)quinazolin-4(3H)-one Derivatives

Li-qiong Zhang, Jia-min Liu, Yi-yuan Gan, Li-hui Shao, Yi-hong Fu, Zhen-chao Wang,* and Gui-ping Ouyang*

*College of Pharmacy, Guizhou University, Huaxi St., Guiyang 550025, China

Abstract

A series of novel 2-(2-(phenoxy)pyridin-3-yl)quinazolin-4(3H)-one derivatives were designed, synthesized as antitumor agents. The antitumor activities of target compounds were evaluated and compared with positive drug Gefitinib employing standard MTT assay against A549 (human lung adenocarcinoma cell), PC-3 (prostate cancer cells), K562 (human chronic myeloid leukemia cells), HepG2 (human liver cancer cell) cancer cell lines in vitro. The pharmacological screening results revealed that many compounds exhibited moderate levels of antitumor activities against four cancer cell lines, especially 6-chloro-2-(2-(3,5-dimethylphenoxy)pyridin-3-yl)-3,8-dimethylquinazolin-4(3H)-one (z8) displayed promising activities against A549 (IC50 = 12.47±2.86 μM) than Gefitinib (IC50 = 17.37±6.01 μM). The mechanism and the apoptosis inducing effect of z8 against A549 cell line were studied. The results showed that z8 could inhibit migration and motility of cancer cells, induce cell apoptosis and exhibit the typical apoptotic morphology.