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

Julia Cianci; Jonathan B Baell; Bernard L Flynn; Robert W Gable; Jorgen A Mould; Dharam Paul; Andrew J Harvey

doi:10.1016/j.bmcl.2008.01.099

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

Bioorg Med Chem Lett. 2008 Mar 15;18(6):2055-61. doi: 10.1016/j.bmcl.2008.01.099. Epub 2008 Jan 31.

Authors

Julia Cianci¹, Jonathan B Baell, Bernard L Flynn, Robert W Gable, Jorgen A Mould, Dharam Paul, Andrew J Harvey

Affiliation

¹ The Walter and Eliza Hall Institute of Medical Research, Biotechnology Centre, 4 Research Avenue, La Trobe R&D Park, Bundoora, Vic. 3086, Australia.

PMID: 18289849
DOI: 10.1016/j.bmcl.2008.01.099

Abstract

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.

Publication types

Evaluation Study
Research Support, Non-U.S. Gov't

MeSH terms

Benzofurans / pharmacology
Chalcones / chemical synthesis*
Chalcones / chemistry
Chalcones / pharmacology*
Crystallography, X-Ray
Electrophysiology
Humans
Kv1.3 Potassium Channel / antagonists & inhibitors*
Kv1.3 Potassium Channel / metabolism
Models, Chemical
Molecular Structure
Potassium Channel Blockers / chemical synthesis*
Potassium Channel Blockers / chemistry
Potassium Channel Blockers / pharmacology*
Structure-Activity Relationship

Substances

Benzofurans
Chalcones
Kv1.3 Potassium Channel
Potassium Channel Blockers
khellinone