title: Alpha-keto amides as inhibitors of histone deacetylase.
abstract: Alpha-keto ester and amides were found to be potent inhibitors of histone deacetylase. Nanomolar inhibitors against the isolated enzyme and sub-micromolar inhibitors of cellular proliferation were obtained. The alpha-keto amide 30 also exhibited significant anti-tumor effects in an in vivo tumor model.
authors.affiliation: Cancer Research, Abbott Laboratories, Department R47J, Bldg. AP10, 100 Abbott Park Road, Abbott Park, IL 60064, USA. carol.wada@abbott.com
authors.forename: Carol K
authors.initials: CK
authors.lastname: Wada
authors.forename: Robin R
authors.initials: RR
authors.lastname: Frey
authors.forename: Zhiqin
authors.initials: Z
authors.lastname: Ji
authors.forename: Michael L
authors.initials: ML
authors.lastname: Curtin
authors.forename: Robert B
authors.initials: RB
authors.lastname: Garland
authors.forename: James H
authors.initials: JH
authors.lastname: Holms
authors.forename: Junling
authors.initials: J
authors.lastname: Li
authors.forename: Lori J
authors.initials: LJ
authors.lastname: Pease
authors.forename: Jun
authors.initials: J
authors.lastname: Guo
authors.forename: Keith B
authors.initials: KB
authors.lastname: Glaser
authors.forename: Patrick A
authors.initials: PA
authors.lastname: Marcotte
authors.forename: Paul L
authors.initials: PL
authors.lastname: Richardson
authors.forename: Shannon S
authors.initials: SS
authors.lastname: Murphy
authors.forename: Jennifer J
authors.initials: JJ
authors.lastname: Bouska
authors.forename: Paul
authors.initials: P
authors.lastname: Tapang
authors.forename: Terrance J
authors.initials: TJ
authors.lastname: Magoc
authors.forename: Daniel H
authors.initials: DH
authors.lastname: Albert
authors.forename: Steven K
authors.initials: SK
authors.lastname: Davidsen
authors.forename: Michael R
authors.initials: MR
authors.lastname: Michaelides
mesh_terms: D000577:Amides / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D045744:Cell Line, Tumor; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D056572:Histone Deacetylase Inhibitors; D006655:Histone Deacetylases / Q000378:metabolism; D006801:Humans; D051379:Mice; D023041:Xenograft Model Antitumor Assays / Q000379:methods
chemical_list: D000577:Amides; D004791:Enzyme Inhibitors; D056572:Histone Deacetylase Inhibitors; D006655:Histone Deacetylases