Synthesis and anticancer activities of novel 1,2,4-triazolo[3,4-a] phthalazine derivatives

被引：57

作者：

Xue, Deng-Qi ^{[1
]}

Zhang, Xu-Yao ^{[1
]}

Wang, Chao-Jie ^{[1
]}

Ma, Li-Ying ^{[1
]}

Zhu, Nan ^{[1
]}

He, Peng ^{[1
]}

Shao, Kun-Peng ^{[1
]}

Chen, Peng-Ju ^{[1
]}

Gu, Yi-Fei ^{[1
]}

Zhang, Xiao-Song ^{[1
]}

Wang, Cai-Feng ^{[1
]}

Ji, Cong-Hui ^{[1
]}

Zhang, Qiu-Rong ^{[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 / 85卷

关键词：

Triazole; Phthalazine; Anticancer; Apoptosis; Cell cycle arrest; ANTIPROLIFERATIVE ACTIVITY; VATALANIB; DESIGN; 1,2,3-TRIAZOLE; ANTAGONISTS; INHIBITION; RESISTANT; ANALOGS;

D O I：

10.1016/j.ejmech.2014.07.031

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Trying to develop potent and selective anticancer agents, two series of novel 1,2,4-triazolo[3,4-a] phthalazine derivatives were designed and synthesized. Their antitumor activities were evaluated by MU method against four selected human cancer cell lines (MGC-803, EC-9706, HeLa and MCF-7). Our results showed that compound 11h exhibited good anticancer activities compared to 5-fluorouracil against the four tested cell lines, with IC50 values ranging from 2.0 to 4.5 mu M. Flow cytometry analysis indicated that compound 11h induced the cellular early apoptosis and cell cycle arrest at G2/M phase in EC-9706. (C) 2014 Published by Elsevier Masson SAS.

引用

页码：235 / 244

页数：10

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