Chin. J. Org. Chem. ›› 2013, Vol. 33 ›› Issue (05): 1026-1034.DOI: 10.6023/cjoc201211052 Previous Articles     Next Articles

Articles

水杨酰芳胺类化合物的设计、合成及体外抗肿瘤活性研究

王杰a, 邬皓a, 李家明a, 许勤龙a, 何广卫b, 钟国琛a, 张艳春a   

  1. a 安徽中医学院药学院 安徽省现代中药重点实验室 合肥 230031;
    b 合肥医工医药有限公司 合肥 230059
  • 收稿日期:2012-12-03 修回日期:2013-01-15 发布日期:2013-01-21
  • 通讯作者: 李家明,lijiaming2004@sina.com E-mail:lijiaming2004@sina.com
  • 基金资助:

    安徽省自然科学基金(No. 1208085MH128)、国家创新药物孵化基地(No. 2012ZX09401066)资助项目

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

Wang Jiea, Wu Haoa, Li Jiaminga, Xu Qinlonga, He Guangweib, Zhong Guochena, Zhang Yanchuna   

  1. a Anhui Key Laboratory of Traditional Chinese Medicine, Department of Pharmacy, Anhui College of Traditional Chinese Medicine, Hefei 230031;
    b Hefei Medical Engineering Pharmaceutical Co, Ltd., Hefei 230059
  • Received:2012-12-03 Revised:2013-01-15 Published:2013-01-21

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, 1H NMR, 13C 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.

Key words: N-aryl-salicylamide, tyrosine kinase inhibitors, antitumor