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

2007; Elsevier BV; Volume: 18; Issue: 4 Linguagem: Inglês

10.1016/j.bmcl.2007.12.057

1464-3405

Sylvie Fréchette, Silvana Leit, Soon Hyung Woo, Guillaume Lapointe, Guillaume Jeannotte, Oscar Moradei, Isabelle Paquin, Giliane Bouchain, Stéphane Raeppel, Frédéric Gaudette, Nancy Zhou, Arkadii Vaisburg, Marielle Fournel, Pu Yan, Marie-Claude Trachy-Bourget, Ann Kalita, Marie‐France Robert, Aihua Lu, Jubrail Rahil, A. Robert MacLeod, Jeffrey M. Besterman, Zuomei Li, Daniel Delorme,

Peptidase Inhibition and Analysis

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.