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

被引：102

作者：

Ma, Li-Ying ^{[1
]}

Pang, Lu-Ping ^{[1
]}

Wang, Bo ^{[1
]}

Zhang, Miao ^{[1
]}

Hu, Biao ^{[1
]}

Xue, Deng-Qi ^{[1
]}

Shao, Kun-Peng ^{[1
]}

Zhang, Bao-Le ^{[1
]}

Liu, Ying ^{[1
]}

Zhang, En ^{[1
]}

Liu, Hong-Min ^{[1
]}

机构：

[1] Zhengzhou Univ, Sch Pharmaceut Sci, New Drug Res & Dev Ctr, Zhengzhou 450001, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 86卷

基金：

中国国家自然科学基金;

关键词：

Triazole; Pyrimidine; Anticancer; Apoptosis; Cell cycle arrest; ANTIPROLIFERATIVE ACTIVITY; ANTIFUNGAL ACTIVITY; INHIBITORS; NUCLEOSIDES; DERIVATIVES;

D O I：

10.1016/j.ejmech.2014.08.010

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2014 Published by Elsevier Masson SAS.

引用

页码：368 / 380

页数：13

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