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

OV Yarishkin, HW Ryu, JY Park, MS Yang…

文献索引：Yarishkin, Oleg V.; Ryu, Hyung Won; Park, Jae-Yong; Yang, Min Suk; Hong, Seong-Geun; Park, Ki Hun Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 1 p. 137 - 140

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被引用次数: 51

摘要

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 μM) was the most potent K+ channel blocker.