Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors

[Image: see text] The V600E mutation of B-Raf kinase results in constitutive activation of the MAPK signaling pathway and is present in approximately 7% of all cancers. Using structure-based design, a novel series of pyrazolopyridine inhibitors of B-Raf(V600E) was developed. Optimization led to the...

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Detalhes bibliográficos
Main Authors: Wenglowsky, Steve, Ren, Li, Ahrendt, Kateri A., Laird, Ellen R., Aliagas, Ignacio, Alicke, Bruno, Buckmelter, Alex J., Choo, Edna F., Dinkel, Victoria, Feng, Bainian, Gloor, Susan L., Gould, Stephen E., Gross, Stefan, Gunzner-Toste, Janet, Hansen, Joshua D., Hatzivassiliou, Georgia, Liu, Bonnie, Malesky, Kim, Mathieu, Simon, Newhouse, Brad, Raddatz, Nicholas J., Ran, Yingqing, Rana, Sumeet, Randolph, Nikole, Risom, Tyler, Rudolph, Joachim, Savage, Scott, Selby, LeAnn T., Shrag, Michael, Song, Kyung, Sturgis, Hillary L., Voegtli, Walter C., Wen, Zhaoyang, Willis, Brandon S., Woessner, Richard D., Wu, Wen-I, Young, Wendy B., Grina, Jonas
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2011
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4017973/
https://ncbi.nlm.nih.gov/pubmed/24900315
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml200025q
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