Issue 1, 2012
From the journal:

MedChemComm

Click JAHAs: conformationally restricted ferrocene-based histone deacetylase inhibitors†‡

John Spencer,*a   Jahangir Amin,a   Ramesh Boddiboyena,a   Graham Packham,b   Breeze E. Cavell,b   Sharifah S. Syed Alwi,b   Ronald M. Paranal,c   Tom D. Heightman,§d   Minghua Wang,d   Brian Marsden,d   Peter Coxhead,e   Matthew Guille,e   Graham J. Tizzard,f   Simon J. Colesf  and  James E. Bradner.c  

* Corresponding authors

a School of Science, University of Greenwich at Medway, Chatham, UK
E-mail: j.spencer@gre.ac.uk
Fax: +44-2083319805
Tel: +44-2083318215

b Cancer Research UK Centre, University of Southampton, Faculty of Medicine, Mailpoint 824, Southampton General Hospital, Tremona Road, Southampton, UK

c Dana-Farber Cancer Institute, 44 Binney Street, Dana Building, D510D, Boston, USA

d Structural Genomics Consortium, University of Oxford, Old Road Campus Research Building, Old Road Campus, Roosevelt Drive, Headington, Oxford, UK

e School of Biological Sciences, King Henry Building, University of Portsmouth, Portsmouth, UK

f UK National Crystallography Service, School of Chemistry, University of Southampton, Highfield, Southampton, UK

Abstract

A small library of ferrocene-based 1,2,3-triazole-containing hydroxamic acids has been synthesised employing click chemistry: 7-(4-ferrocenyl-1H-1,2,3-triazol-1-yl)-N-hydroxyheptanamide, 4b, containing the 1,2,3-triazole moiety adjacent to the ferrocene group, displayed excellent HDAC inhibition and activity in cells, inhibiting the deacetylation of tubulin as well as inducing cell cycle arrest.

Graphical abstract: Click JAHAs: conformationally restricted ferrocene -based histone deacetylase inhibitors

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Article information

DOI
https://doi.org/10.1039/C1MD00203A
Article type
Concise Article
Submitted
06 Aug 2011
Accepted
28 Sep 2011
First published
20 Oct 2011

Med. Chem. Commun., 2012,3, 61-64

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Click JAHAs: conformationally restricted ferrocene-based histone deacetylase inhibitors

J. Spencer, J. Amin, R. Boddiboyena, G. Packham, B. E. Cavell, S. S. Syed Alwi, R. M. Paranal, T. D. Heightman, M. Wang, B. Marsden, P. Coxhead, M. Guille, G. J. Tizzard, S. J. Coles and J. E. Bradner., Med. Chem. Commun., 2012, 3, 61 DOI: 10.1039/C1MD00203A

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