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

AbstractA 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, compound11k showed the most potent cytotoxicity against PC-3 cells (IC50 = 5.59 ± 0.78 μM). Compound11k also significantly inhibited the colony formation and migration of PC-3 cells. Meanwhile, compound11k 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 compound11k might be a valuable lead compound for anti-tumor agents targeting prostate cancer cells.
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research