Synthesis, structure–activity relationships and preliminary antitumor evaluation of benzothiazole-2-thiol derivatives as novel apoptosis inducers

A series of novel benzothiazole-2-thiol derivatives were synthesized, and their anti-proliferative activities on HepG2 and MCF-7 cells were investigated. Most compounds had inhibitory effects on cell growth, and some of them were more effective than cisplatin. Compounds 6m and 6t displayed good inhibitory activities against a panel of different types of human cancer cell lines, with IC50 values in the low micromolar range. Further biological evaluation indicated that 6m induced apoptosis in HepG2 cancer cells. Structure–activity relationships were also proposed.

Graphical abstractA series of novel benzothiazole-2-thiol derivatives were synthesized and evaluated for antitumor. The most potent compound 6m exhibited good inhibitory activities against a panel of different types of human cancer cell lines with IC50 values in the low micromolar range and induced apoptosis in HepG2 cancer cells.Figure optionsDownload full-size imageDownload as PowerPoint slide