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

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

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Received: 22 February 2012 / Revised: 20 March 2012 / Accepted: 26 March 2012 / Published: 30 March 2012
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Abstract

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.
Keywords: anticancer; synthesis; apoptosis; benzothiazole-2-thiol derivatives anticancer; synthesis; apoptosis; benzothiazole-2-thiol derivatives
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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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