Literature DB >> 25994553

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

Rob De Vreese1, Nicholas Van Steen, Tom Verhaeghe, Tom Desmet, Nadia Bougarne, Karolien De Bosscher, Veronick Benoy, Wanda Haeck, Ludo Van Den Bosch, Matthias D'hooghe.   

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.

Entities:  

Mesh：

Substances：

Year:  2015        PMID： 25994553     DOI： 10.1039/c5cc03295d

Source DB:  PubMed          Journal:  Chem Commun (Camb)        ISSN： 1359-7345            Impact factor:   6.222


  7 in total

1.  Design, synthesis and evaluation of antiproliferative activity of melanoma-targeted histone deacetylase inhibitors.

Authors:  Idris Raji; Kabir Ahluwalia; Adegboyega K Oyelere
Journal:  Bioorg Med Chem Lett       Date:  2017-01-17       Impact factor: 2.823

2.  Why Hydroxamates May Not Be the Best Histone Deacetylase Inhibitors--What Some May Have Forgotten or Would Rather Forget?

Authors:  Sida Shen; Alan P Kozikowski
Journal:  ChemMedChem       Date:  2015-11-25       Impact factor: 3.466

Review 3.  A patent review of histone deacetylase 6 inhibitors in neurodegenerative diseases (2014-2019).

Authors:  Sida Shen; Alan P Kozikowski
Journal:  Expert Opin Ther Pat       Date:  2019-12-25       Impact factor: 6.674

4.  Glucocorticoid Receptor-mediated transactivation is hampered by Striatin-3, a novel interaction partner of the receptor.

Authors:  Ioanna Petta; Nadia Bougarne; Jolien Vandewalle; Lien Dejager; Sofie Vandevyver; Marlies Ballegeer; Sofie Desmet; Jonathan Thommis; Lode De Cauwer; Sam Lievens; Claude Libert; Jan Tavernier; Karolien De Bosscher
Journal:  Sci Rep       Date:  2017-08-21       Impact factor: 4.379

5.  Exploration of thiaheterocyclic hHDAC6 inhibitors as potential antiplasmodial agents.

Authors:  Rob De Vreese; Carmen de Kock; Peter J Smith; Kelly Chibale; Matthias D'hooghe
Journal:  Future Med Chem       Date:  2017-03-06       Impact factor: 3.808

6.  Development of Improved HDAC6 Inhibitors as Pharmacological Therapy for Axonal Charcot-Marie-Tooth Disease.

Authors:  Veronick Benoy; Pieter Vanden Berghe; Matthew Jarpe; Philip Van Damme; Wim Robberecht; Ludo Van Den Bosch
Journal:  Neurotherapeutics       Date:  2017-04       Impact factor: 7.620

7.  HDAC6 is a therapeutic target in mutant GARS-induced Charcot-Marie-Tooth disease.

Authors:  Veronick Benoy; Lawrence Van Helleputte; Robert Prior; Constantin d'Ydewalle; Wanda Haeck; Natasja Geens; Wendy Scheveneels; Begga Schevenels; M Zameel Cader; Kevin Talbot; Alan P Kozikowski; Pieter Vanden Berghe; Philip Van Damme; Wim Robberecht; Ludo Van Den Bosch
Journal:  Brain       Date:  2018-03-01       Impact factor: 13.501
  7 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.