Design, synthesis and in vitro biological evaluation of novel [1,2,3]triazolo[4,5-d]pyrimidine derivatives containing a thiosemicarbazide moiety

被引：29

作者：

Geng, Peng-Fei ^{[1
]}

Liu, Xue-Qi ^{[1
]}

Zhao, Tao-Qian ^{[1
]}

Wang, Cong-Cong ^{[1
]}

Li, Zhong-Hua ^{[1
]}

Zhang, Ji ^{[1
]}

Wei, Hao-Ming ^{[1
]}

Hu, Biao ^{[1
]}

Ma, Li-Ying ^{[1
]}

Liu, Hong-Min ^{[1
]}

机构：

[1] Zhengzhou Univ, Collaborat Innovat Ctr New Drug Res & Safety Eval, Minist Educ,Sch Pharmaceut Sci, Key Lab Henan Prov Drug Qual & Evaluat,Key Lab Te, Zhengzhou 450001, Henan, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2018年 / 146卷

基金：

中国国家自然科学基金;

关键词：

Triazole; Pyrimidine; Thiosemicarbazide; Antiproliferative activity; POTENTIAL ANTICANCER AGENTS; ANTIPROLIFERATIVE AGENTS; FLOW-CYTOMETRY; HYBRIDS; INHIBITORS; APOPTOSIS; BCL-2; ASSAY;

D O I：

10.1016/j.ejmech.2018.01.031

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of hybrid molecules containing [1,2,3]triazolo[4,5-d]pyrimidine and thiosemicarbazide moieties were designed, synthesized and evaluated for their antiproliferative activities against MGC-803, NCI-H1650 and PC-3 human cancer cells. Some of the synthesized compounds showed moderate to good activity against three selected cancer cell lines. Among these compounds, compound 29 displayed the most potent antiproliferative activity as well as good selectivity between cancer cells and normal cells. Further mechanism studies revealed that compound 29 could obviously inhibit the colony formation and migration of MGC-803 as well as induced apoptosis. (C) 2018 Elsevier Masson SAS. All rights reserved.

引用

页码：147 / 156

页数：10

共 33 条

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