Synthesis and Biological Evaluation of Novel Benzothiazole-2-thiol Derivatives as Potential Anticancer Agents
| Autor: | Yong Xia, Xuan-Hong Shi, Tinghong Ye, Zhao Wang, Youzhi Xu, Mei Deng, Yuquan Wei, Luoting Yu |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2012 |
| Předmět: |
synthesis
Stereochemistry Pharmaceutical Science Antineoplastic Agents anticancer Article Analytical Chemistry lcsh:QD241-441 chemistry.chemical_compound benzothiazole-2-thiol derivatives lcsh:Organic chemistry Cell Line Tumor Drug Discovery Humans Benzothiazoles Physical and Theoretical Chemistry IC50 Biological evaluation apoptosis Cell Proliferation chemistry.chemical_classification Dose-Response Relationship Drug Organic Chemistry Benzothiazole chemistry Chemistry (miscellaneous) Apoptosis Cell culture Cancer cell Thiol Molecular Medicine Human cancer |
| Zdroj: | Molecules, Vol 17, Iss 4, Pp 3933-3944 (2012) Molecules Molecules; Volume 17; Issue 4; Pages: 3933-3944 |
| ISSN: | 1420-3049 |
| Popis: | 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 (IC(50) = 1.2 nM), SW620 (IC(50) = 4.3 nM), A549 (IC(50) = 44 nM) and HepG2 (IC(50) = 48 nM) and was found to induce apoptosis in HepG2 cancer cells. |
| Databáze: | OpenAIRE |
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