Eleven novel 4‐anilinoquinazoline derivatives were synthesized and evaluated for their in vitro antiproliferative activity. Among them, compound 9a exhibited the best potency, with IC₅₀ values of 25−682 nm against various types of cancer cell lines. In addition, 9a was confirmed that it could arrest the cell cycle at G₂/M phase and trigger apoptosis. Indirect immunofluorescence staining revealed its antitubulin property. Importantly, 9a significantly inhibited tumor growths in SM‐7721 xenograft models (57.0% tumor mass change) without causing significant loss of body weight, suggesting that 9a is a promising new anticancer agent to be developed.

中文翻译：

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新型取代的4-苯胺基喹唑啉类抗肿瘤药的合成及生物评价

合成了11种新颖的4-苯胺基喹唑啉衍生物，并对其体外抗增殖活性进行了评估。其中，化合物9a表现出最佳效能，对各种类型的癌细胞系的IC ₅₀值为25-682 n m。另外，证实9a可以阻止细胞周期处于G ₂ / M期并触发细胞凋亡。间接免疫荧光染色显示其抗微管蛋白特性。重要的是，9a可以显着抑制SM‐7721异种移植模型中的肿瘤生长（肿瘤质量改变为57.0％），而不会引起体重的显着降低，这表明9a 是有前途的新型抗癌药。