Design, synthesis and antitumor activity evaluation of cinnamamide-containing benzamides derivatives
LU Bing-liu
WU Xia-bing
YAO Kai
LI Jian-qi
ZHANG Qing-wei
Abstract：Objective:To synthesize novel cinnamamide-containing benzamides derivatives and evaluate their antitumor activities.Methods:Hybrids (5a ～5q) of CI-994 and cinnamamide analogues have been designed,and synthesized through 3 steps using substituted cinnamamides.Results:Seventeen designed compounds were synthesized and characterized by 1H-NMR and HRMS.In vitro biological studies showed that most of the compounds exhibited inhibitory activity against HDAC1,among which compound 5q showed similar activity compared with CI-994.Antitumor cell proliferation experiment in vitro showed that compound 5q with significant selectivity over MRC-5 human normal cell lines (IC50 ＞ 50 μmol· L-1) demonstrated better antiproliferative potency than CI-994 against Hut78 cells,A549 cells,U-937 cells and PC-3 cells.Conclusion:Compound 5q which demonstrated significant antiproliferative potency against cancer cells and inhibitory activity against HDAC1 is worth of much more research.
Keywords：cinnamamidehistone deacetylases (HDACs)drug designantitumor activity
Publication Date：2018-02-15
Online Publishing Date：2026-08-14(First online date of this platform, not the publication date of the document)
Pages：6( 345-350 )