Chimeric microtubule disruptors

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

Research output: Contribution to journalArticlepeer-review

23 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)2907-2909
JournalChemical Communications
Volume46
Issue number17
DOIs
Publication statusPublished - 7 May 2010

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