Details

Autor(en) / Beteiligte

• De Vreese, Rob
• Van Steen, Nicholas
• Verhaeghe, Tom
• Desmet, Tom
• Bougarne, Nadia
• De Bosscher, Karolien
• Benoy, Veronick
• Haeck, Wanda
• Van Den Bosch, Ludo
• D'hooghe, Matthias

Titel

Synthesis of benzothiophene-based hydroxamic acids as potent and selective HDAC6 inhibitorsElectronic supplementary information (ESI) available: Synthetic procedures, spectral data, bioassay results, ligand docking data. See DOI: 10.1039/c5cc03295d

Erscheinungsjahr

2015-06

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• 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. A small library of 3-[(4-hydroxycarbamoylphenyl)aminomethyl]benzothiophenes was prepared, leading to the identification of three representatives as potent and selective HDAC6 inhibitors.