期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 64, 期 -, 页码 99-110出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.03.058
关键词
1,2,3-Triazole; Dithiocarbamate; Urea; Hybrid; Antiproliferative; Apoptosis
资金
- National Natural Science Foundation of China [81172937, U1204206]
- China Postdoctoral Science Foundation [20100480857, 201104402]
- New Teachers' Fund for Doctor Stations, Ministry of Education [20114101120013]
A series of novel 1,2,3-triazole-dithiocarbamate-urea hybrids were designed, synthesized and their antiproliferative activities against four selected human cancer cell lines were evaluated. The results showed that a number of the hybrids exhibited potent activity in selected human cancer cell lines. Among them, compounds 27 and 34 showed broad spectrum anticancer activity with IC50 values ranging from 1.62 to 20.84 mu M and 0.76 to 13.55 mu M, respectively. Interestingly, compounds 27 and 34, being very potent against MGC-803 cells, exhibited no significant cytotoxicity against normal human embryonic kidney cells at up to 55 mu M and 70 mu M, respectively. Evidences of cell cycle arrest and apoptosis induction were obtained for the most effective compounds 27 and 34 by means of flow cytometry and microscopic techniques. (C) 2013 Elsevier Masson SAS. All rights reserved.
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