Design and synthesis of novel 1,2,3-triazole-pyrimidine hybrids as potential anticancer agents

作者：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; Liu, Hong-Min^*

来源：European Journal of Medicinal Chemistry, 2014, 86: 368-380.

DOI：10.1016/j.ejmech.2014.08.010

• Triazole
• Pyrimidine
• Anticancer
• Apoptosis
• Cell cycle arrest

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 IC50 values ranging from 1.42 to 6.52 mu M. 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.

• 出版日期2014-10-30
• 单位郑州大学