Inhibiting VEGFR-2 has been set up as a therapeutic strategy for treatment of cancer. Thus, nineteen new quinazoline-4(3H)-one derivatives were designed and synthesized. Preliminary cytotoxicity studies of the synthesized compounds were evaluated against three human cancer cell lines (HepG-2, MCF-7 and HCT-116) using MTT assay method. Doxorubicin and sorafenib were used as positive controls. Five compounds were found to have promising cytotoxic activities against all cell lines. Compound 16_f, containing a 2-chloro-5-nitrophenyl group, has emerged as the most active member. It was approximately 4.39-, 5.73- and 1.96-fold more active than doxorubicin and 3.88-, 5.59- and 1.84-fold more active than sorafenib against HepG2, HCT-116 and MCF-7 cells, respectively. The most active cytotoxic agents were further evaluated in vitro for their VEGFR-2 inhibitory activities. The results of in vitro VEGFR-2 inhibition were consistent with that of the cytotoxicity data. Molecular docking of these compounds into the kinase domain, moreover, supported the results.

抑制 VEGFR-2 已被确立为治疗癌症的治疗策略。因此，设计并合成了19 种新的喹唑啉-4(3 H )-one 衍生物。使用 MTT 分析方法对合成的化合物对三种人类癌细胞系（HepG-2、MCF-7 和 HCT-116）的初步细胞毒性研究进行了评估。多柔比星和索拉非尼用作阳性对照。发现五种化合物对所有细胞系都具有良好的细胞毒活性。化合物16 _f含有一个 2-氯-5-硝基苯基，已成为最活跃的成员。它对 HepG2、HCT-116 和 MCF-7 细胞的活性分别比阿霉素高约 4.39、5.73 和 1.96 倍，比索拉非尼高 3.88、5.59 和 1.84 倍。最活跃的细胞毒性剂在体外进一步评估了它们的 VEGFR-2 抑制活性。体外VEGFR-2 抑制的结果与细胞毒性数据的结果一致。此外，这些化合物与激酶结构域的分子对接支持了结果。