1. Design and synthesis of novel 1,2,3-triazole-pyrimidine hybrids as potential anticancer agents.
- Author
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Ma, Li-Ying, Pang, Lu-Ping, Wang, Bo, Zhang, Miao, Hu, Biao, Xue, Deng-Qi, Shao, Kun-Peng, Zhang, Bao-Le, Liu, Ying, Zhang, En, and Liu, Hong-Min
- Subjects
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PYRIMIDINES , *DRUG design , *ANTINEOPLASTIC agent synthesis , *CANCER cells , *CELL lines , *APOPTOSIS - Abstract
A series of novel 1,2,3-triazole-pyrimidine hybrids were designed, synthesized and evaluated for their anticancer activity against four selected cancer cell lines (MGC-803, EC-109, MCF-7 and B16-F10). Most of the synthesized compounds exhibited moderate to good activity against all the cancer cell lines selected. Compound 17 showed the most excellent anticancer activity with single-digit micromolar IC 50 values ranging from 1.42 to 6.52 μM. Further mechanism studies revealed that compound 17 could obviously inhibit the proliferation of EC-109 cancer cells by inducing apoptosis and arresting the cell cycle at G2/M phase. [ABSTRACT FROM AUTHOR]
- Published
- 2014
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