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

Molecules

Xuan-Hong Shi¹  Zhao Wang¹  Yong Xia¹  Ting-Hong Ye¹  Mei Deng¹  You-Zhi Xu¹  Yu-Quan Wei¹ 

[1] id="af1-molecules-17-03933">State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, Chi

关键词: anticancer;    synthesis;    apoptosis;    benzothiazole-2-thiol derivatives;   

DOI  :  10.3390/molecules17043933

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2012 by the authors; licensee MDPI, Basel, Switzerland.