1. Design and synthesis of novel 1,2,3-triazole-dithiocarbamate hybrids as potential anticancer agents
- Author
-
Duan, Ying-Chao, Ma, Yong-Cheng, Zhang, En, Shi, Xiao-Jing, Wang, Meng-Meng, Ye, Xian-Wei, and Liu, Hong-Min
- Subjects
- *
DRUG design , *DITHIOCARBAMATES synthesis , *DRUG development , *ANTINEOPLASTIC agents , *CANCER cell culture , *FLUOROURACIL , *FLOW cytometry - Abstract
Abstract: 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 μM and 0.49–12.45 μM, 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. [Copyright &y& Elsevier]
- Published
- 2013
- Full Text
- View/download PDF