Synthesis and biological evaluation of chalcones as inhibitors of the voltage-gated potassium channel Kv1.3

• Published in: Bioorganic & medicinal chemistry Vol. 18; no. 6; pp. 2055 - 2061
• Main Authors: Cianci, Julia, Baell, Jonathan B., Flynn, Bernard L., Gable, Robert, W., Mould, Jorgen A., Paul, Dharam, Harvey, Andrew J.
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 15-03-2008; Elsevier
• Subjects: Benzofurans - pharmacology; Biological and medical sciences; Chalcones; Chalcones - chemical synthesis; Chalcones - chemistry; Chalcones - pharmacology; Conformational analysis; Crystallography, X-Ray; Electrophysiology; Humans; Ion channel blockers; Kv1.3; Kv1.3 Potassium Channel - antagonists & inhibitors; Kv1.3 Potassium Channel - metabolism; Medical sciences; Miscellaneous; Models, Chemical; Molecular modelling; Molecular Structure; Natural product derivatives; Pharmacology. Drug treatments; Potassium Channel Blockers - chemical synthesis; Potassium Channel Blockers - chemistry; Potassium Channel Blockers - pharmacology; Structure-Activity Relationship; X-ray crystallography; X-ray crystallography; Chalcones; Molecular modelling; Conformational analysis; Electrophysiology; Kv1.3; Natural product derivatives; Ion channel blockers; Potassium channel antagonist; Ionic channel; Natural compound; X ray diffraction; Flavonoid; Modeling; Biological activity; Molecular model; Inhibitor; Benzofuran derivatives; Chemical synthesis
• ISSN: 0960-894X; 0968-0896; 1464-3405; 1464-3391
• DOI: 10.1016/j.bmcl.2008.01.099

Chalcone derivatives of the natural product khellinone were synthesised and screened for bioactivity against the voltage-gated potassium channel Kv1.3. X-ray crystallography was employed to investigate relationships between the structure and function of a selection of the reported chalcones.