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Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation

Bromodomain-containing protein 4 (BRD4) represents a promising drug target for anti-inflammatory therapeutics. Herein, we report the design, synthesis, and pharmacological evaluation of novel chromone derivatives via scaffold hopping to discover a new class of orally bioavailable BRD4-selective inhi...

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Detalhes bibliográficos
Publicado no:J Med Chem
Main Authors: Liu, Zhiqing, Chen, Haiying, Wang, Pingyuan, Li, Yi, Wold, Eric A., Leonard, Paul G., Joseph, Sarah, Brasier, Allan R., Tian, Bing, Zhou, Jia
Formato: Artigo
Idioma:Inglês
Publicado em: 2020
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC7989030/
https://ncbi.nlm.nih.gov/pubmed/32255647
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.0c00035
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