Issue 4, 2004
From the journal:

Organic & Biomolecular Chemistry

Polymer-assisted, multi-step solution phase synthesis and biological screening of histone deacetylase inhibitors

Akanksha Bapna,a   Emma Vickerstaffe,b   Brian H. Warrington,b   Mark Ladlow,*b   Tai-Ping D. Fan*a  and  Steven V. Ley*c  

* Corresponding authors

a Department of Pharmacology, University of Cambridge, Tennis Court Road, Cambridge, UK

b GlaxoSmithKline Cambridge Technology Centre, University Chemical Laboratory, Lensfield Road, Cambridge, UK
E-mail: Mark.2.Ladlow@gsk.com
Fax: +44 (0)1223 331532
Tel: +44 (0)1223 336349

c Department of Chemistry, University Chemical Laboratory, Lensfield Road, Cambridge, UK

Abstract

The polymer-assisted solution phase synthesis (PASP) of an array of histone deacetylase (HDAc) inhibitors is described. HDAc inhibitors have considerable potential as new anti-proliferative agents. Selected compounds were shown to inhibit both human endothelial cell proliferation, and the formation of tubules (neovascularisation) in an in vitro model of angiogenesis.

Graphical abstract: Polymer-assisted, multi-step solution phase synthesis and biological screening of histone deacetylase inhibitors

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Article information

DOI
https://doi.org/10.1039/B313414H
Article type
Paper
Submitted
24 Oct 2003
Accepted
16 Dec 2003
First published
27 Jan 2004

Org. Biomol. Chem., 2004,2, 611-620

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Polymer-assisted, multi-step solution phase synthesis and biological screening of histone deacetylase inhibitors

A. Bapna, E. Vickerstaffe, B. H. Warrington, M. Ladlow, T. D. Fan and S. V. Ley, Org. Biomol. Chem., 2004, 2, 611 DOI: 10.1039/B313414H

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