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• Shi, X
• Wang, Z
• Xia, Y
• Ye, T
• Deng, M
• Xu, Y
• Wei, Y
• Yu, L
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• Shi, X
• Wang, Z
• Xia, Y
• Ye, T
• Deng, M
• Xu, Y
• Wei, Y
• Yu, L
• [+] on PubMed
• Shi, X
• Wang, Z
• Xia, Y
• Ye, T
• Deng, M
• Xu, Y
• Wei, Y
• Yu, L

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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

Xuan-Hong Shi, Zhao Wang, Yong Xia, Ting-Hong Ye, Mei Deng, You-Zhi Xu, Yu-Quan Wei and Luo-Ting Yu*

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; in revised form: 20 March 2012 / Accepted: 26 March 2012 / Published: 30 March 2012

Download PDF Full-Text [278 KB, uploaded 30 March 2012 10:29 CEST]

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

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