title: Structure-activity relationships of aryloxyalkanoic acid hydroxyamides as potent inhibitors of histone deacetylase.
abstract: Syntheses of aryloxyalkanoic acid hydroxyamides are described, all of which are potent inhibitors of histone deacetylase, some being more potent in vitro than trichostatin A (IC(50)=3 nM). Variation of the substituents on the benzene ring as well as fusion of a second ring have marked effects on potency, in vitro IC(50) values down to 1 nM being obtained.
authors.affiliation: Department of Chemistry, University College London, Christopher Ingold Laboratories, 20 Gordon Street, London WC1H OAJ, UK. c.m.marson@ucl.ac.uk
authors.forename: Charles M
authors.initials: CM
authors.lastname: Marson
authors.forename: Thevaki
authors.initials: T
authors.lastname: Mahadevan
authors.forename: Jon
authors.initials: J
authors.lastname: Dines
authors.forename: Stéphane
authors.initials: S
authors.lastname: Sengmany
authors.forename: James M
authors.initials: JM
authors.lastname: Morrell
authors.forename: John P
authors.initials: JP
authors.lastname: Alao
authors.forename: Simon P
authors.initials: SP
authors.lastname: Joel
authors.forename: David M
authors.initials: DM
authors.lastname: Vigushin
authors.forename: R
authors.initials: R
authors.lastname: Charles Coombes
mesh_terms: D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D056572:Histone Deacetylase Inhibitors; D006655:Histone Deacetylases / Q000737:chemistry; D006801:Humans; D011487:Protein Conformation; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D056572:Histone Deacetylase Inhibitors; D006655:Histone Deacetylases