Sulfonate chalcone as new class voltage-dependent K+ channel blocker

Oleg V Yarishkin; Hyung Won Ryu; Jae-Yong Park; Min Suk Yang; Seong-Geun Hong; Ki Hun Park

doi:10.1016/j.bmcl.2007.10.114

Sulfonate chalcone as new class voltage-dependent K+ channel blocker

Bioorg Med Chem Lett. 2008 Jan 1;18(1):137-40. doi: 10.1016/j.bmcl.2007.10.114. Epub 2007 Nov 4.

Authors

Oleg V Yarishkin¹, Hyung Won Ryu, Jae-Yong Park, Min Suk Yang, Seong-Geun Hong, Ki Hun Park

Affiliation

¹ Department of Physiology, School of Medicine and Institute of Health Science, Gyeongsang National University, Jinju 660-701, Republic of Korea.

PMID: 18032041
DOI: 10.1016/j.bmcl.2007.10.114

Abstract

Chalcone derivatives 1-17 were synthesized and their voltage-dependent K+ channel inhibitory activities were investigated. The effective K+ channel blockers were shown to be sulfonate chalcones 9-17, in which the sulfonyloxy group is placed on the A-ring. The 3'-(p-aminobenzene-sulfonylhydroxy)-4-hydroxychalcone 17 (IC50 = 0.51+/-0.05 microM) was the most potent K+ channel blocker.

Publication types

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

MeSH terms

Alkanesulfonates / chemistry*
Alkanesulfonates / pharmacology*
Animals
CHO Cells
Chalcones / chemistry*
Chalcones / pharmacology*
Cricetinae
Cricetulus
Dose-Response Relationship, Drug
Potassium Channel Blockers / chemistry*
Potassium Channel Blockers / pharmacology*
Potassium Channels / drug effects
Potassium Channels / metabolism

Substances

Alkanesulfonates
Chalcones
Potassium Channel Blockers
Potassium Channels