Journal
MOLECULES
Volume 17, Issue 4, Pages 3933-3944Publisher
MDPI
DOI: 10.3390/molecules17043933
Keywords
anticancer; synthesis; apoptosis; benzothiazole-2-thiol derivatives
Funding
- National Science and Technology Major Project of China [2009ZX09103-132]
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A series of novel benzothiazole-2-thiol derivatives were synthesized and their structures determined by H-1-NMR, C-13-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.
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