Chimeric microtubule disruptors

Research output: Contribution to journalArticle

Authors

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

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.

Details

Original languageEnglish
Pages (from-to)2907-9
Number of pages3
JournalChemical Communications
Volume46
Issue number17
Publication statusPublished - 2010