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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 publication

DOI

10.1039/c002558e

Type

Journal article

Journal

Chem Commun (Camb)

Publication Date

07/05/2010

Volume

46

Pages

2907 - 2909

Keywords

Animals, Antineoplastic Agents, Binding Sites, Carbonic Anhydrase II, Carbonic Anhydrase Inhibitors, Cell Line, Tumor, Computer Simulation, Crystallography, X-Ray, Humans, Ligands, Mice, Mice, Nude, Tubulin Modulators, Xenograft Model Antitumor Assays