Journal of Hebei University(Natural Science Edition) >

2018 , Vol. 38 >Issue 2: 140 - 146

DOI: https://doi.org/10.3969/j.issn.1000-1565.2018.02.005

Synthesis and in vitro antitumor activity of N-(2-aminophenyl)-4-cinnamamidobenzamide

  • PENG Xiaoran ,
  • WU Jianong ,
  • FU Wentao ,
  • LI Shenghui ,
  • WANG Shuxiang
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  • Key Laboratory of Chemical Biology of Hebei Province, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, College of Chemistry and Environmental Science, Hebei University, Baoding 071002, China

Received date: 2017-12-25

  Online published: 2018-03-25

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Abstract

A series of benzamide(3a-3j)histone deacetylase inhibitors(HDACi)were synthesized.Their activity for inhibiting histone deacetylase(HDAC)and in vitro cytotoxicity against MCF-7,HeLa,and A549 cell lines were determined by fluorescence analysis and MTT assay.The 2-substituted N-(2-aminophenyl)-4-cinnamamidobenzamides 3b and 3e exhibited high cytotoxicity and activity of inhibiting HDAC.The IC50 value of 3b and 3e for HDAC inhibition were 7.71 and 3.5 μmol/L,and closed to that of chidamide(2.7 μmol/L).The IC50 value of 3b against MCF-7,HeLa,and A549 cell lines were 6.5,6.0,and 5.6 μmol/L;that of 3e against MCF-7,HeLa,and A549 cell lines were 3.9,3.1,and 2.9 μmol/L.The in vitro cytotoxicity of 3b and 3e is closed to that of MS-275(3.5 μmol/L).

Key words： N-(2-aminophenyl)-4-cinnamamidobenzamide; histone deacetylase inhibitor; cytotoxicity

Cite this article

PENG Xiaoran , WU Jianong , FU Wentao , LI Shenghui , WANG Shuxiang . Synthesis and in vitro antitumor activity of N-(2-aminophenyl)-4-cinnamamidobenzamide[J]. Journal of Hebei University(Natural Science Edition), 2018 , 38(2) : 140 -146 . DOI: 10.3969/j.issn.1000-1565.2018.02.005

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