title: Design and synthesis of a novel class of histone deacetylase inhibitors.
abstract: Histone deacetylase inhibitors (HDACs) have emerged as a novel class of antiproliferative agents. Utilizing structure-based design, the synthesis of a series of sulfonamide hydroxamic acids is described. Further optimization of this series by substitution of the terminal aromatic ring yielded HDAC inhibitors with good in vitro and in vivo activities.
authors.affiliation: Department of Medicinal Chemistry, MethylGene Inc., 7220 Frederick-Banting, Montréal, Québec, Canada H4S 2A1.
authors.forename: R
authors.initials: R
authors.lastname: Lavoie
authors.forename: G
authors.initials: G
authors.lastname: Bouchain
authors.forename: S
authors.initials: S
authors.lastname: Frechette
authors.forename: S H
authors.initials: SH
authors.lastname: Woo
authors.forename: E
authors.initials: E
authors.lastname: Abou-Khalil
authors.forename: S
authors.initials: S
authors.lastname: Leit
authors.forename: M
authors.initials: M
authors.lastname: Fournel
authors.forename: P T
authors.initials: PT
authors.lastname: Yan
authors.forename: M C
authors.initials: MC
authors.lastname: Trachy-Bourget
authors.forename: C
authors.initials: C
authors.lastname: Beaulieu
authors.forename: Z
authors.initials: Z
authors.lastname: Li
authors.forename: J
authors.initials: J
authors.lastname: Besterman
authors.forename: D
authors.initials: D
authors.lastname: Delorme
mesh_terms: D002455:Cell Division / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D056572:Histone Deacetylase Inhibitors; D006801:Humans; D066298:In Vitro Techniques; D008958:Models, Molecular
chemical_list: D004791:Enzyme Inhibitors; D056572:Histone Deacetylase Inhibitors