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Title: Chimeric microtubule disruptors. Author: Leese MP, Jourdan F, Kimberley MR, Cozier GE, Thiyagarajan N, Stengel C, Regis-Lydi S, Foster PA, Newman SP, Acharya KR, Ferrandis E, Purohit A, Reed MJ, Potter BV. Journal: Chem Commun (Camb); 2010 May 07; 46(17):2907-9. PubMed ID: 20386818. 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.[Abstract] [Full Text] [Related] [New Search]