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

Rob De Vreese | Zendy; Nicholas Van Steen | Zendy; Tom Verhaeghe | Zendy; Tom Desmet | Zendy; Nadia Bougarne | Zendy; Karolien De Bosscher | Zendy; Veronick Benoy | Zendy; Wanda Haeck | Zendy; Ludo Van Den Bosch | Zendy; Matthias D’hooghe | Zendy

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

Author(s) -

Rob De Vreese,

Nicholas Van Steen,

Tom Verhaeghe,

Tom Desmet,

Nadia Bougarne,

Karolien De Bosscher,

Veronick Benoy,

Wanda Haeck,

Ludo Van Den Bosch,

Matthias D’hooghe

Publication year - 2015

Publication title -

chemical communications

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.837

H-Index - 333

eISSN - 1364-548X

pISSN - 1359-7345

DOI - 10.1039/c5cc03295d

Subject(s) - benzothiophene , hdac6 , chemistry , hydroxamic acid , stereochemistry , combinatorial chemistry , pharmacology , biochemistry , biology , organic chemistry , histone deacetylase , histone , gene , thiophene

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.

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