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

Keyphrases

• Pharmacological Evaluation 100%
• Orally Bioavailable 100%
• Bromodomain-containing Protein 4 (BRD4) 100%
• Inhibitor Scaffold 100%
• Chromone Derivatives 100%
• Optimization Evaluation 100%
• Scaffold Hopping 100%
• Bromodomain 50%
• Selective Inhibitor 33%
• Toll-like 16%
• Murine Model 16%
• High-resolution 16%
• Therapeutic Potential 16%
• Pharmacokinetic Properties 16%
• Synthetic Evaluation 16%
• Inflammatory Genes 16%
• Airway Inflammation 16%
• Inflammatory Diseases 16%
• IC50 Value 16%
• Family Protein 16%
• Drug Target 16%
• Design Evaluation 16%
• Excellent Selectivity 16%
• In Vivo Efficacy 16%
• Binding Affinity 16%
• Co-crystal Structure 16%
• Promising Drug 16%
• Structure Optimization 16%
• In Vivo Inflammation 16%
• Anti-inflammatory Therapeutics 16%

Pharmacology, Toxicology and Pharmaceutical Science

• Chromone Derivative 100%
• Respiratory Tract Inflammation 50%
• Inflammatory Disease 50%
• Anti-Inflammatory Drug 50%
• Murine 50%
• IC50 50%
• Toll Like Receptor 50%
• Pharmacokinetics 50%

Biochemistry, Genetics and Molecular Biology

• Bromodomain 100%
• Binding Affinity 11%
• Protein Family 11%
• Murine 11%
• IC50 11%
• Toll-Like Receptor 11%
• Pharmacokinetic Properties 11%
• Anti-Inflammatory 11%