文献类型：期刊文献

英文题名：Discovery of tetrahydrothiazolopyridine-incorporated curcumol derivatives as novel and highly potent anti-cancer agents

作者：Guo, Shixun[1];Fan, Yuhang[1];Li, Wei[1];Lu, Kailin[1];Wang, Qiang[1];Meng, Chong[1];Tong, Yuxuan[1];Li, Jian[1];Wei, Jinlian[1];Zhang, Yongqiang[1]

机构：[1]East China Univ Sci & Technol, Shanghai Frontiers Sci Ctr Optogenet Tech Cell Met, Sch Pharm, Shanghai Key Lab New Drug Design, Shanghai 200237, Peoples R China

年份：2026

卷号：304

外文期刊名：EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

收录：;WOS:【SCI-EXPANDED(收录号:WOS:001658888900001)】；

基金：Financial support from the program of the National Natural Science Foundation of China (22171080, 22471072, Y.-Q. Z.; 22577030, J.-L. W), Natural Science Foundation of Shanghai Municipality (23ZR1417200, Y.-Q. Z.) is gratefully acknowledged.

语种：英文

摘要：Herein, the structural modification of curcumol via a privileged scaffold incorporation strategy has been demonstrated, which enables the production of a class of novel tetrahydrothiazolopyridine-containing derivatives. Among them, the analogs with an ortho-or meta-substituted benzoyl exhibited superior in vitro anti-proliferative activity, and 9b with a 2, 3-dimethylbenzoyl group showed the most potent activity and good selectivity. Furthermore, 9b showed good in vivo anti-cancer activity and could efficiently suppress the migration of cancer cells, while no apparent toxicity was observed. Further mechanistic studies revealed that 9b exhibited an ability to induce G2/M-phase arrest in cancer cells associated with the disruption of tubulin polymerization. In particular, 9b could efficiently repress self-renewal of cancer stem cells. Overall, our findings highlight 9b as a promising lead compound in cancer therapy.