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

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  • 作者:Yu Fuqiang, Xu Ying, Wang Hao, Chi Lingling, Si Xiaojie, Gao Chao, Dai Honglin, Liu Limin, Wang Zhengjie, Ke Yu, Liu Hongmin, Zhang Qiurong
  • 期刊:MEDICINAL CHEMISTRY RESEARCH
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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.

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