新型1,2,3-三唑-嘧啶杂合物作为潜在抗癌剂的设计与合成
Design and synthesis of novel 1,2,3-triazole-pyrimidine hybrids as potential anticancer agents.
作者信息
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
机构信息
New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, Avenue Kexue, Zhengzhou 450001, PR China.
New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, Avenue Kexue, Zhengzhou 450001, PR China.
出版信息
Eur J Med Chem. 2014 Oct 30;86:368-80. doi: 10.1016/j.ejmech.2014.08.010. Epub 2014 Aug 5.
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 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.
设计、合成了一系列新型1,2,3-三唑-嘧啶杂化物，并对其针对四种选定癌细胞系（MGC-803、EC-109、MCF-7和B16-F10）的抗癌活性进行了评估。大多数合成化合物对所有选定的癌细胞系均表现出中等至良好的活性。化合物17表现出最优异的抗癌活性，其IC50值为个位数微摩尔，范围在1.42至6.52 μM之间。进一步的机制研究表明，化合物17可通过诱导细胞凋亡并将细胞周期阻滞在G2/M期来明显抑制EC-109癌细胞的增殖。
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