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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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
Format: Artigo
Language:Inglês
Published: American Chemical Society 2011
Online Access: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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