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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Gepubliceerd in:J Med Chem
Hoofdauteurs: 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
Formaat: Artigo
Taal:Inglês
Gepubliceerd in: 2018
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Article
Online toegang: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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