Structure-Based Discovery of CF53 as a Potent and Orally Bioavailable Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitor

We report structure-based discovery of CF53 (28) as a highly potent and orally active inhibitor of bromodomain and extra-terminal (BET) proteins. By incorporation of a NH-pyrazole group into the 9H-pyrimido[4,5-b]indole core, we identified a series of compounds, that bind to BRD4 BD1 protein with Ki...

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Publicado no:J Med Chem
Main Authors: Zhao, Yujun, Zhou, Bing, Bai, Longchuan, Liu, Liu, Yang, Chao-Yie, Meagher, Jennifer L., Stuckey, Jeanne A., McEachern, Donna, Przybranowski, Sally, Wang, Mi, Ran, Xu, Aguilar, Angelo, Hu, Yang, Kampf, Jeff W., Li, Xiaoqin, Zhao, Ting, Li, Siwei, Wen, Bo, Sun, Duxin, Wang, Shaomeng
Formato: Artigo
Idioma:Inglês
Publicado em: 2018
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6489120/
https://ncbi.nlm.nih.gov/pubmed/30015487
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.8b00483
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