Title of article
4-(Heteroarylaminomethyl)-N-(2-aminophenyl)-benzamides and their analogs as a novel class of histone deacetylase inhibitors
Author/Authors
Sylvie Frechette، نويسنده , , Silvana Leit، نويسنده , , Soon Hyung Woo، نويسنده , , Guillaume Lapointe، نويسنده , , Guillaume Jeannotte، نويسنده , , Oscar Moradei، نويسنده , , Isabelle Paquin، نويسنده , , Giliane Bouchain، نويسنده , , Stéphane Raeppel، نويسنده , , Frédéric Gaudette، نويسنده , , Nancy Zhou، نويسنده , , Arkadii Vaisburg، نويسنده , , Marielle Fournel، نويسنده , , Pu Theresa Yan، نويسنده , , Marie-Claude Trachy-Bourget، نويسنده , , Ann Kalita، نويسنده , , Marie-France Robert، نويسنده , , Aihua Lü، نويسنده , , Jubrail Rahil، نويسنده , , A. Robert MacLeod، نويسنده , , et al.، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
1502
To page
1506
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 IC50 values below the micromolar range, induce hyperacetylation of histones, upregulate expression of the tumor suppressor p21WAF1/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.
Keywords
benzamides , anticancer agents , MGCD0103 , HDAC , Histone deacetylase inhibitors
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799195
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