Synthesis and biological evaluation of novel 2-(2-arylmethylene)hydrazinyl-4-aminoquinazoline derivatives as potent antitumor agents

被引：26

作者：

Jiang, Nan ^{[1
]}

Zhai, Xin ^{[1
]}

Zhao, Yanfang ^{[1
]}

Liu, Yajing ^{[1
]}

Qi, Baohui ^{[1
]}

Tao, Haiyan ^{[1
]}

Gong, Ping ^{[1
]}

机构：

[1] Shenyang Pharmaceut Univ, Sch Pharmaceut Engn, Key Lab New Drugs Design & Discovery Liaoning Pro, Shenyang 110016, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 54卷

关键词：

2-(2-arylmethylene)hydrazinyl-4-aminoquinazoline; Synthesis; Cytotoxicity; CANCER CELLS; CHLOROQUINE; ANTAGONISTS; DISCOVERY; APOPTOSIS; GROWTH; DESIGN; DRUG;

D O I：

10.1016/j.ejmech.2012.05.039

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Two series of novel 2-(2-arylmethylene)hydrazinyl-4-aminoquinazoline derivatives were synthesized and evaluated for their cytotoxicity against H-460, HT-29, HepG2 and SGC-7901 cancer cell lines in vitro. Most compounds displayed moderate to excellent activity, with IC50 values ranging from 0.015 to 4.09 mu M against all tested cell lines, respectively. The most promising compound 9p (E)-2-(24(1-(2,3-dichlorobenzyl)-1H-imidazol-2-yl)methylene)hydrazinyl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine with IC50 values of 0.031 mu M, 0.015 mu M, 0.53 mu M and 0.58 mu M, which was 4- to 224 times more active than references 10 and Iressa, had emerged as a lead for further structural modifications. (C) 2012 Elsevier Masson SAS. All rights reserved.

引用

页码：534 / 541

页数：8

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