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Molecules 2012, 17(4), 3933-3944; doi:10.3390/molecules17043933

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
Author to whom correspondence should be addressed.
Received: 22 February 2012 / Revised: 20 March 2012 / Accepted: 26 March 2012 / Published: 30 March 2012
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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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MDPI and ACS Style

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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