title: Synthesis of benzothiophene-based hydroxamic acids as potent and selective HDAC6 inhibitors.
abstract: A small library of 3-[(4-hydroxycarbamoylphenyl)aminomethyl]benzothiophenes was prepared and assessed as a novel class of HDAC6 inhibitors, leading to the identification of three representatives as potent and selective HDAC6 inhibitors. Further tests with regard to inflammatory responses indicated that HDAC6 inhibition can be uncoupled from transcriptional inhibition at the level of activated NF-κB, AP-1, and GR.
authors.affiliation: SynBioC Research Group, Department of Sustainable Organic Chemistry and Technology, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, B-9000 Ghent, Belgium. matthias.dhooghe@UGent.be.
authors.forename: Rob
authors.initials: R
authors.lastname: De Vreese
authors.forename: Nicholas
authors.initials: N
authors.lastname: Van Steen
authors.forename: Tom
authors.initials: T
authors.lastname: Verhaeghe
authors.forename: Tom
authors.initials: T
authors.lastname: Desmet
authors.forename: Nadia
authors.initials: N
authors.lastname: Bougarne
authors.forename: Karolien
authors.initials: K
authors.lastname: De Bosscher
authors.forename: Veronick
authors.initials: V
authors.lastname: Benoy
authors.forename: Wanda
authors.initials: W
authors.lastname: Haeck
authors.forename: Ludo
authors.initials: L
authors.lastname: Van Den Bosch
authors.forename: Matthias
authors.initials: M
authors.lastname: D'hooghe
mesh_terms: D045744:Cell Line, Tumor; D000073864:Histone Deacetylase 6; D056572:Histone Deacetylase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006655:Histone Deacetylases / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D006877:Hydroxamic Acids / Q000138:chemical synthesis* / Q000737:chemistry; D008958:Models, Molecular; D016328:NF-kappa B / Q000378:metabolism; D013876:Thiophenes / Q000138:chemical synthesis* / Q000737:chemistry; D018808:Transcription Factor AP-1 / Q000378:metabolism; D014404:Tubulin / Q000378:metabolism
chemical_list: D056572:Histone Deacetylase Inhibitors; D006877:Hydroxamic Acids; D016328:NF-kappa B; D013876:Thiophenes; D018808:Transcription Factor AP-1; D014404:Tubulin; C088015:benzothiophene; C433811:HDAC6 protein, human; D000073864:Histone Deacetylase 6; D006655:Histone Deacetylases