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.

中文翻译：

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2-（2-（苯氧基）吡啶-3-基）喹唑啉-4（3）的合成及生物学性质评价

设计了一系列新型的2-（2-（苯氧基）吡啶-3-基）喹唑啉-4（3H ）-衍生物，合成了其作为抗肿瘤药。评价了目标化合物的抗肿瘤活性，并与标准药物吉非替尼（Gefitinib）进行了标准MTT检测，针对A549（人肺腺癌细胞），PC-3（前列腺癌细胞），K562（人慢性髓性白血病细胞），HepG2（人肝癌）进行了比较细胞）的癌细胞系中的体外。药理筛选结果表明，许多化合物对四种癌细胞，特别是6-氯-2-（2-（3-（3,5-二甲基苯氧基）吡啶-3-基）-3,8-二甲基喹唑啉-具有中等水平的抗肿瘤活性。 4（3 H ）-一（z8 ）显示有希望的活动针对A549（IC 50 = 12.47±2.86μM）比吉非替尼（IC 50 = 17.37±6.01 μM ）。研究了z8对A549细胞株的作用机制及其诱导凋亡的作用。结果表明，z8可以抑制癌细胞的迁移和运动，诱导细胞凋亡，并表现出典型的凋亡形态。