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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Veröffentlicht in:	Chemical communications (Cambridge, England) England), 2010-01, Vol.46 (17), p.2907-2909
Hauptverfasser:	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:	Artikel
Sprache:	eng
Schlagworte:	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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Beschreibung
Zusammenfassung:	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