Issue 17, 2010
From the journal:

Chemical Communications

Chimeric microtubule disruptors†

Mathew P. Leese,a   Fabrice Jourdan,a   Meriel R. Kimberley,a   Gyles E. Cozier,a   Nethaji Thiyagarajan,b   Chloe Stengel,c   Sandra Regis-Lydi,d   Paul A. Foster,c   Simon P. Newman,c   K. Ravi Acharya,b   Eric Ferrandis,d   Atul Purohit,c   Michael J. Reed‡c  and  Barry V. L. Potter*a  

* Corresponding authors

a Medicinal Chemistry & Sterix Ltd., Department of Pharmacy & Pharmacology, University of Bath, Claverton Down, Bath, UK
E-mail: B.V.L.Potter@bath.ac.uk
Fax: +44 (0)1225-386114
Tel: +44 (0)1225-386639

b Department of Biology & Biochemistry, University of Bath, Claverton Down, Bath, UK

c Department of Endocrinology & Metabolic Medicine & Sterix Ltd., Imperial College London, St Mary's Hospital, London W2 1NY, UK

d Institut de Recherche Henri Beaufour, 91966 Les Ulis Cedex, France

Abstract

A chimeric approach is used to discover microtubule disruptors with excellent in vitro activity and oral bioavailability; a ligand–protein interaction with carbonic anhydrase that enhances bioavailability is characterised by protein X-ray crystallography. Dosing of a representative chimera in a tumour xenograft model confirms the excellent therapeutic potential of the class.

Graphical abstract: Chimeric microtubule disruptors

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Article information

DOI
https://doi.org/10.1039/C002558E
Article type
Communication
Submitted
08 Feb 2010
Accepted
04 Mar 2010
First published
20 Mar 2010

Chem. Commun., 2010,46, 2907-2909

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Chimeric microtubule disruptors

M. P. Leese, F. Jourdan, M. R. Kimberley, G. E. Cozier, N. Thiyagarajan, C. Stengel, S. Regis-Lydi, P. A. Foster, S. P. Newman, K. R. Acharya, E. Ferrandis, A. Purohit, M. J. Reed and B. V. L. Potter, Chem. Commun., 2010, 46, 2907 DOI: 10.1039/C002558E

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