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Substituted N-(2-aminophenyl)-benzamides, (E)-N-(2-aminophenyl)-acrylamides and their analogues: Novel classes of histone deacetylase inhibitors

2006; Elsevier BV; Volume: 16; Issue: 15 Linguagem: Inglês

10.1016/j.bmcl.2006.05.005

1464-3405

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

Epigenetics and DNA Methylation

Inhibition of histone deacetylases (HDACs) is emerging as a new strategy in human cancer therapy. Novel 2-aminophenyl benzamides and acrylamides, that can inhibit human HDAC enzymes and induce hyperacetylation of histones in human cancer cells, have been designed and synthesized. These compounds selectively inhibit proliferation and cause cell cycle arrest in various human cancer cells but not in normal cells. The growth inhibition of 2-aminophenyl benzamides and acrylamides against human cancer cells in vitro is reversible and is dependent on the induction of histone acetylation. Compounds of this class can significantly reduce tumor growth in human tumor xenograft models.