Discovery of Benzotriazolo[4,3-d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains

[Image: see text] Inhibition of the bromodomains of the BET family, of which BRD4 is a member, has been shown to decrease myc and interleukin (IL) 6 in vivo, markers that are of therapeutic relevance to cancer and inflammatory disease, respectively. Herein we report substituted benzo[b]isoxazolo[4,5...

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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: Taylor, Alexander M., Vaswani, Rishi G., Gehling, Victor S., Hewitt, Michael C., Leblanc, Yves, Audia, James E., Bellon, Steve, Cummings, Richard T., Côté, Alexandre, Harmange, Jean-Christophe, Jayaram, Hari, Joshi, Shivangi, Lora, Jose M., Mertz, Jennifer A., Neiss, Adrianne, Pardo, Eneida, Nasveschuk, Christopher G., Poy, Florence, Sandy, Peter, Setser, Jeremy W., Sims, Robert J., Tang, Yong, Albrecht, Brian K.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2015
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4753545/
https://ncbi.nlm.nih.gov/pubmed/26985289
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml500411h
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