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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Опубликовано в: :J Med Chem
Главные авторы: 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
Формат: Artigo
Язык:Inglês
Опубликовано: 2018
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Article
Online-ссылка: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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