Design, synthesis and antitumor activity evaluation of 4,6,7-trisubstituted quinazoline derivatives containing benzothiazole moiety

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 (IC 50  = 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.