Sulfonate chalcone as new class voltage-dependent K+ channel blocker.
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.
Yarishkin
Oleg V
OV
Department of Physiology, School of Medicine and Institute of Health Science, Gyeongsang National University, Jinju 660-701, Republic of Korea.
Ryu
Hyung Won
HW
Park
Jae-Yong
JY
Yang
Min Suk
MS
Hong
Seong-Geun
SG
Park
Ki Hun
KH
D000476:Alkanesulfonates / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D016466:CHO Cells; D047188:Chalcones / Q000737:chemistry* / Q000494:pharmacology*; D006224:Cricetinae; D003412:Cricetulus; D004305:Dose-Response Relationship, Drug; D026902:Potassium Channel Blockers / Q000737:chemistry* / Q000494:pharmacology*; D015221:Potassium Channels / Q000187:drug effects / Q000378:metabolism
D000476:Alkanesulfonates; D047188:Chalcones; D026902:Potassium Channel Blockers; D015221:Potassium Channels