Design, Synthesis, and Biological Evaluation of N-Aryl-salicylamide Derivatives as Potential Antitumor Agents

被引：5

作者：

Wang, Jie ^{[1
]}

Wu, Hao ^{[1
]}

Li, Jiaming ^{[1
]}

Xu, Qinlong ^{[1
]}

He, Guangwei ^{[2
]}

Zhong, Guochen ^{[1
]}

Zhang, Yanchun ^{[1
]}

机构：

[1] Anhui Coll Tradit Chinese Med, Dept Pharm, Anhui Key Lab Tradit Chinese Med, Hefei 230031, Peoples R China

[2] Hefei Med Engn Pharmaceut Co Ltd, Hefei 230059, Peoples R China

来源：

CHINESE JOURNAL OF ORGANIC CHEMISTRY | 2013年 / 33卷 / 05期

关键词：

N-aryl-salicylamide; tyrosine kinase inhibitors; antitumor; TYROSINE KINASE; SALICYLANILIDES; INHIBITORS; DRUGS;

D O I：

10.6023/cjoc201211052

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

According to the scaffold hopping, a series of N-aryl-salicylamide derivatives, which have fragments of tyrosine kinase inhibitors lapatinib and neratinib were designed and synthesized. Their structures were identified by IR, H-1 NMR, C-13 NMR and MS techniques. The target compounds were tested for cytotoxic activity against four cancer cell lines, including A549, MCF-7, SGC-7901, Bel-7402, by methyl thiazolyl tetrazolium (MTT) in vitro. All the compounds demonstrated certain antitumor abilities, and some of them were better than gefitinib.

引用

页码：1026 / 1034

页数：9

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