Article

4-(Heteroarylaminomethyl)-N-(2-aminophenyl)-benzamides and their analogs as a novel class of histone deacetylase inhibitors.

MethylGene Inc., Department of Medicinal Chemistry, 7220 Frederick-Banting, Montréal, QC, Canada.
Bioorganic & medicinal chemistry letters (impact factor: 2.65). 03/2008; 18(4):1502-6. DOI:10.1016/j.bmcl.2007.12.057
Source: PubMed

ABSTRACT The synthesis and biological evaluation of a variety of 4-(heteroarylaminomethyl)-N-(2-aminophenyl)-benzamides and their analogs is described. Some of these compounds were shown to inhibit HDAC1 with IC(50) values below the micromolar range, induce hyperacetylation of histones, upregulate expression of the tumor suppressor p21(WAF1/Cip1), and inhibit proliferation of human cancer cells. In addition, certain compounds of this class were active in several human tumor xenograft models in vivo.

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Keywords

certain compounds
 
compounds
 
HDAC1
 
human tumor xenograft models
 
induce hyperacetylation
 
proliferation
 
tumor suppressor p21(WAF1/Cip1)
 
upregulate expression
 

Sylvie Fréchette