21714-54-5Relevant 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.
