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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Autori principali: 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
Natura: Artigo
Lingua:Inglês
Pubblicazione: American Chemical Society 2011
Accesso online: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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