1186223-07-3Relevant academic research and scientific papers
Imidazo[4,5-b]pyridine inhibitors of B-Raf kinase
Newhouse, Bradley J.,Wenglowsky, Steve,Grina, Jonas,Laird, Ellen R.,Voegtli, Walter C.,Ren, Li,Ahrendt, Kateri,Buckmelter, Alex,Gloor, Susan L.,Klopfenstein, Nathalie,Rudolph, Joachim,Wen, Zhaoyang,Li, Xianfeng,Feng, Bainian
, p. 5896 - 5899 (2013/10/22)
This Letter details the synthesis and evaluation of imidazo[4,5-b]pyridines as inhibitors of B-Raf kinase. These compounds bind in a DFG-in, αC-helix out conformation of B-Raf, which is a binding mode associated with significant kinase selectivity. Structure-activity relationship studies involved optimization of the ATP-cleft binding region of these molecules, and led to compound 23, an inhibitor with excellent enzyme/cell potency, and kinase selectivity.
IMDIZO [4. 5-B] PYRIDINE DERIVATIVES USED AS RAF INHIBITORS
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Page/Page column 55, (2009/10/22)
Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
