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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Veröffentlicht in:	Journal of medicinal chemistry 2020-05, Vol.63 (10), p.5242-5256
Hauptverfasser:	Liu, Zhiqing, Chen, Haiying, Wang, Pingyuan, Li, Yi, Wold, Eric A, Leonard, Paul G, Joseph, Sarah, Brasier, Allan R, Tian, Bing, Zhou, Jia
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Biological Availability Cell Cycle Proteins - antagonists & inhibitors Cell Cycle Proteins - metabolism Cell Line, Transformed Chromones - administration & dosage Chromones - chemistry Chromones - pharmacology Crystallization - methods Crystallization - trends Drug Discovery - methods Drug Discovery - trends Drug Evaluation, Preclinical - methods Humans Male Mice Mice, Inbred C57BL Protein Structure, Secondary Protein Structure, Tertiary Structure-Activity Relationship Transcription Factors - antagonists & inhibitors Transcription Factors - metabolism
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