Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 62, Issue -, Pages 11-19Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.12.046
Keywords
1,2,3-triazole; Dithiocarbamate; Hybrid; Anticancer; Cell cycle arrest; Apoptosis
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Funding
- National Natural Science Foundation of China [81172937, U1204206]
- China Postdoctoral Science Foundation [20100480857, 201104402]
- New Teachers' Fund for Doctor Stations, Ministry of Education [20114101120013]
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A series of novel 1,2,3-triazole-dithiocarbamate hybrids were designed, synthesized and evaluated for anticancer activity against four selected human tumor cell lines (MGC-803, MCF-7, PC-3, EC-109). Majority of the synthesized compounds exhibited moderate to potent activity against MGC-803 and MCF-7. Among them, compounds 3a and 3c showed excellent broad spectrum anticancer activity with IC50 values ranging from 0.73 to 11.61 mu M and 0.49-12.45 mu M, respectively. Particularly, compound 3a was more potent than 5-fluorouracil against all tested human cancer cell lines. Flow cytometry analysis demonstrated that treatment of MGC-803 with 3c led to cell cycle arrest at G2/M phase accompanied by an increase in apoptotic cell death after 12 h. (C) 2013 Elsevier Masson SAS. All rights reserved.
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