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Bioorg Med Chem Lett ; 14(3): 783-6, 2004 Feb 09.
Article in English | MEDLINE | ID: mdl-14741289

ABSTRACT

Bis-aryl ureas have been disclosed previously as a potent class of Raf kinase inhibitors. Modifications in the amide portion led to an improvement in aqueous solubility, an important characteristic for an oral drug. Based on this finding, we hypothesize that this portion of the molecule is directed towards the solvent in Raf-1.


Subject(s)
Enzyme Inhibitors/pharmacology , MAP Kinase Kinase Kinase 1 , Proto-Oncogene Proteins c-raf/antagonists & inhibitors , Urea/analogs & derivatives , Urea/pharmacology , Amides/chemical synthesis , Amides/pharmacology , Baculoviridae/genetics , Enzyme Inhibitors/chemical synthesis , Humans , MAP Kinase Kinase Kinases/antagonists & inhibitors , Molecular Structure , Pyridines/chemistry , Pyridines/pharmacology , Recombinant Proteins/antagonists & inhibitors , Solubility , Structure-Activity Relationship , Urea/chemical synthesis
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