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

被引：88

作者：

Ma, Li-Ying ^{[1
]}

Wang, Bo ^{[1
]}

Pang, Lu-Ping ^{[1
]}

Zhang, Miao ^{[1
]}

Wang, Sai-Qi ^{[1
]}

Zheng, Yi-Chao ^{[1
]}

Shao, Kun-Peng ^{[1
]}

Xue, Deng-Qi ^{[1
]}

Liu, Hong-Min ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2015年 / 25卷 / 05期

基金：

中国国家自然科学基金;

关键词：

Pyrimidine; Urea; Triazole; Anticancer; Apoptosis; ANTIPROLIFERATIVE ACTIVITY; BIOLOGICAL EVALUATION; CLICK CHEMISTRY; INHIBITORS; ANALOGS; 1,2,3-TRIAZOLES; NUCLEOSIDES; DERIVATIVES; DISCOVERY;

D O I：

10.1016/j.bmcl.2014.12.087

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-urea hybrids were designed, synthesized and evaluated for anticancer activity against four selected cancer cell lines (MGC-803, EC-109, MCF-7 and B16-F10). Majority of the synthesized compounds exhibited moderate to potent activity against all the cancer cell lines assayed. Particularly, compounds 26, 30 and 38 exhibited excellent growth inhibition against B16-F10 with IC50 values of 32 nM, 35 nM and 42 nM, respectively. Flow cytometry analysis demonstrated that compound 26 induced the cellular apoptosis in a concentration-dependent manner. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：1124 / 1128

页数：5

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