Chimeric microtubule disruptors

• DOI: 10.1039/c002558e
• Publication Date: 2010-03-21T09:30:23Z
• Authors: 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
• Keywords: Chimera (genetics)

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