A series of novel 4,6,7-trisubstituted quinazoline derivatives containing benzothiazole moiety were designed, synthesized and evaluated for their antitumor activity against four human cancer cells (PC-3, MGC-803, A549 and Eca-109) using MTT assay. Among them, compound 11k showed the most potent cytotoxicity against PC-3 cells (IC₅₀ = 5.59 ± 0.78 μM). Compound 11k also significantly inhibited the colony formation and migration of PC-3 cells. Meanwhile, compound 11k induced cell cycle arrest at S-phase and cell apoptosis, as well as increased accumulation of intracellular reactive oxygen species. All the findings suggest that compound 11k might be a valuable lead compound for anti-tumor agents targeting prostate cancer cells.

设计、合成了一系列含有苯并噻唑部分的新型4,6,7-三取代喹唑啉衍生物，并使用MTT法评估了它们对四种人类癌细胞（PC-3、MGC-803、A549和Eca-109）的抗肿瘤活性。其中，化合物11k对PC-3细胞表现出最强的细胞毒性（IC ₅₀  = 5.59 ± 0.78 μM）。化合物11k还显着抑制PC-3细胞的集落形成和迁移。同时，化合物11k诱导细胞周期停滞在S期和细胞凋亡，并增加细胞内活性氧的积累。所有研究结果表明化合物11k可能是针对前列腺癌细胞的抗肿瘤药物的一种有价值的先导化合物。