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Synthesis and Biological Evaluation of Novel Benzothiazole-2-thiol Derivatives as Potential Anticancer Agents

State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China
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Molecules 2012, 17(4), 3933-3944; https://doi.org/10.3390/molecules17043933
Received: 22 February 2012 / Revised: 20 March 2012 / Accepted: 26 March 2012 / Published: 30 March 2012
A series of novel benzothiazole-2-thiol derivatives were synthesized and their structures determined by 1H-NMR, 13C-NMR and HRMS (ESI). The effects of all compounds on a panel of different types of human cancer cell lines were investigated. Among them, pyridinyl-2-amine linked benzothiazole-2-thiol compounds 7d, 7e, 7f and 7i exhibited potent and broad-spectrum inhibitory activities. Compound 7e displayed the most potent anticancer activity on SKRB-3 (IC50 = 1.2 nM), SW620 (IC50 = 4.3 nM), A549 (IC50 = 44 nM) and HepG2 (IC50 = 48 nM) and was found to induce apoptosis in HepG2 cancer cells. View Full-Text
Keywords: anticancer; synthesis; apoptosis; benzothiazole-2-thiol derivatives anticancer; synthesis; apoptosis; benzothiazole-2-thiol derivatives
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Shi, X.-H.; Wang, Z.; Xia, Y.; Ye, T.-H.; Deng, M.; Xu, Y.-Z.; Wei, Y.-Q.; Yu, L.-T. Synthesis and Biological Evaluation of Novel Benzothiazole-2-thiol Derivatives as Potential Anticancer Agents. Molecules 2012, 17, 3933-3944.

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