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

doi:10.3969/j.issn.1000-1565.2018.02.005

Abstract

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 IC₅₀value 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

CLC Number:

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.

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