Structure-Based Discovery of 4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole (CD161) as a Potent and Orally Bioavailable BET Bromodomain Inhibitor

We have designed and synthesized 9H-pyrimido[4,5-b]indole-containing compounds to obtain potent and orally bioavailable BET inhibitors. By incorporation of an indole or a quinoline moiety to the 9H-pyrimido[4,5-b]indole core, we identified a series of small molecules showing high binding affinities...

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Publicado en:J Med Chem
Main Authors: Zhao, Yujun, Bai, Longchuan, Liu, Liu, McEachern, Donna, Stuckey, Jeanne A., Meagher, Jennifer L., Yang, Chao-Yie, Ran, Xu, Zhou, Bing, Hu, Yang, Li, Xiaoqin, Wen, Bo, Zhao, Ting, Li, Siwei, Sun, Duxin, Wang, Shaomeng
Formato: Artigo
Idioma:Inglês
Publicado: 2017
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Article
Acceso en liña:https://ncbi.nlm.nih.gov/pmc/articles/PMC6993113/
https://ncbi.nlm.nih.gov/pubmed/28463487
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.7b00193
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