Articles

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

  • Wang Jie ,
  • Wu Hao ,
  • Li Jiaming ,
  • Xu Qinlong ,
  • He Guangwei ,
  • Zhong Guochen ,
  • Zhang Yanchun
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  • 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 date: 2012-12-03

  Revised date: 2013-01-15

  Online published: 2013-01-21

Abstract

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.

Cite this article

Wang Jie , Wu Hao , Li Jiaming , Xu Qinlong , He Guangwei , Zhong Guochen , Zhang Yanchun . Design, Synthesis, and Biological Evaluation of N-Aryl-salicylamide Derivatives as Potential Antitumor Agents[J]. Chinese Journal of Organic Chemistry, 2013 , 33(05) : 1026 -1034 . DOI: 10.6023/cjoc201211052

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