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Issue 48, 2015
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Synthesis of benzothiophene-based hydroxamic acids as potent and selective HDAC6 inhibitors

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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.

Graphical abstract: Synthesis of benzothiophene-based hydroxamic acids as potent and selective HDAC6 inhibitors

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Publication details

The article was received on 23 Apr 2015, accepted on 11 May 2015 and first published on 11 May 2015


Article type: Communication
DOI: 10.1039/C5CC03295D
Citation: Chem. Commun., 2015,51, 9868-9871

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    Synthesis of benzothiophene-based hydroxamic acids as potent and selective HDAC6 inhibitors

    R. De Vreese, N. Van Steen, T. Verhaeghe, T. Desmet, N. Bougarne, K. De Bosscher, V. Benoy, W. Haeck, L. Van Den Bosch and M. D'hooghe, Chem. Commun., 2015, 51, 9868
    DOI: 10.1039/C5CC03295D

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