title: Substituted N-(2-aminophenyl)-benzamides, (E)-N-(2-aminophenyl)-acrylamides and their analogues: novel classes of histone deacetylase inhibitors.
abstract: 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.
authors.affiliation: MethylGene Inc., Department of Medicinal Chemistry, 7220 Frederick-Banting, Montréal, QC, Canada H4S 2A1. moradeio@methylgene.com
authors.forename: Oscar
authors.initials: O
authors.lastname: Moradei
authors.forename: Silvana
authors.initials: S
authors.lastname: Leit
authors.forename: Nancy
authors.initials: N
authors.lastname: Zhou
authors.forename: Sylvie
authors.initials: S
authors.lastname: Fréchette
authors.forename: Isabelle
authors.initials: I
authors.lastname: Paquin
authors.forename: Stéphane
authors.initials: S
authors.lastname: Raeppel
authors.forename: Frédéric
authors.initials: F
authors.lastname: Gaudette
authors.forename: Giliane
authors.initials: G
authors.lastname: Bouchain
authors.forename: Soon H
authors.initials: SH
authors.lastname: Woo
authors.forename: Arkadii
authors.initials: A
authors.lastname: Vaisburg
authors.forename: Marielle
authors.initials: M
authors.lastname: Fournel
authors.forename: Ann
authors.initials: A
authors.lastname: Kalita
authors.forename: Aihua
authors.initials: A
authors.lastname: Lu
authors.forename: Marie-Claude
authors.initials: MC
authors.lastname: Trachy-Bourget
authors.forename: Pu T
authors.initials: PT
authors.lastname: Yan
authors.forename: Jianhong
authors.initials: J
authors.lastname: Liu
authors.forename: Zuomei
authors.initials: Z
authors.lastname: Li
authors.forename: Jubrail
authors.initials: J
authors.lastname: Rahil
authors.forename: A Robert
authors.initials: AR
authors.lastname: MacLeod
authors.forename: Jeffrey M
authors.initials: JM
authors.lastname: Besterman
authors.forename: Daniel
authors.initials: D
authors.lastname: Delorme
mesh_terms: D000178:Acrylamides / Q000737:chemistry / Q000494:pharmacology*; D001549:Benzamides / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D056572:Histone Deacetylase Inhibitors; D006801:Humans; D013329:Structure-Activity Relationship
chemical_list: D000178:Acrylamides; D001549:Benzamides; D004791:Enzyme Inhibitors; D056572:Histone Deacetylase Inhibitors