Chimeric microtubule disruptors

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 tumo...

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Bibliographic Details
Published in:Chemical communications (Cambridge, England) England), 2010-01, Vol.46 (17), p.2907-2909
Main Authors: Leese, Mathew P, Jourdan, Fabrice, Kimberley, Meriel R, Cozier, Gyles E, Thiyagarajan, Nethaji, Stengel, Chloe, Regis-Lydi, Sandra, Foster, Paul A, Newman, Simon P, Acharya, K Ravi, Ferrandis, Eric, Purohit, Atul, Reed, Michael J, Potter, Barry V L
Format: Article
Language:English
Subjects:
Animals
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Binding Sites
Carbonic Anhydrase II - chemistry
Carbonic Anhydrase II - metabolism
Carbonic Anhydrase Inhibitors - chemical synthesis
Carbonic Anhydrase Inhibitors - chemistry
Carbonic Anhydrase Inhibitors - pharmacology
Cell Line, Tumor
Computer Simulation
Crystallography, X-Ray
Humans
Ligands
Mice
Mice, Nude
Tubulin Modulators - chemistry
Tubulin Modulators - metabolism
Xenograft Model Antitumor Assays
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Summary: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.
ISSN:1359-7345
1364-548X
DOI:10.1039/c002558e