Synthesis and biological evaluation of chalcones as inhibitors of the voltage-gated potassium channel Kv1.3.
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.
Cianci
Julia
J
The Walter and Eliza Hall Institute of Medical Research, Biotechnology Centre, 4 Research Avenue, La Trobe R&D Park, Bundoora, Vic. 3086, Australia.
Baell
Jonathan B
JB
Flynn
Bernard L
BL
Gable
Robert W
RW
Mould
Jorgen A
JA
Paul
Dharam
D
Harvey
Andrew J
AJ
D001572:Benzofurans / Q000494:pharmacology; D047188:Chalcones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D004594:Electrophysiology; D006801:Humans; D051664:Kv1.3 Potassium Channel / Q000037:antagonists & inhibitors* / Q000378:metabolism; D008956:Models, Chemical; D015394:Molecular Structure; D026902:Potassium Channel Blockers / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D001572:Benzofurans; D047188:Chalcones; D051664:Kv1.3 Potassium Channel; D026902:Potassium Channel Blockers; C509273:khellinone