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

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

Research output: Contribution to journal › Article › peer-review

35 Citations (Scopus)

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 μM) was the most potent K⁺ channel blocker.

Original language	English
Pages (from-to)	137-140
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	1
DOIs	https://doi.org/10.1016/j.bmcl.2007.10.114
Publication status	Published - 2008 Jan 1
Externally published	Yes

Keywords

Chalcone
Ion channel
K channel blocker
Potassium channel blocker
Sulfonate chalcone

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

Access to Document

10.1016/j.bmcl.2007.10.114

Cite this

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title = "Sulfonate chalcone as new class voltage-dependent K+ channel blocker",

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 μM) was the most potent K+ channel blocker.",

keywords = "Chalcone, Ion channel, K channel blocker, Potassium channel blocker, Sulfonate chalcone",

author = "Yarishkin, {Oleg V.} and Ryu, {Hyung Won} and Park, {Jae Yong} and Yang, {Min Suk} and Hong, {Seong Geun} and Park, {Ki Hun}",

note = "Funding Information: This work was financially supported by the MOST/KOSEF to the Environmental Biotechnology National Core Research Center (Grant R15-2003-012-02001-0), Korea. Oleg V. Yarishkin was supported by Korea Research Foundation Grant (KRF-2004-005-E00008). Also, Hyung Won Ryu is the recipient of a BK21 fellowship from the Ministry of Education. ",

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T1 - Sulfonate chalcone as new class voltage-dependent K+ channel blocker

AU - Yarishkin, Oleg V.

AU - Ryu, Hyung Won

AU - Park, Jae Yong

AU - Yang, Min Suk

AU - Hong, Seong Geun

AU - Park, Ki Hun

N1 - Funding Information: This work was financially supported by the MOST/KOSEF to the Environmental Biotechnology National Core Research Center (Grant R15-2003-012-02001-0), Korea. Oleg V. Yarishkin was supported by Korea Research Foundation Grant (KRF-2004-005-E00008). Also, Hyung Won Ryu is the recipient of a BK21 fellowship from the Ministry of Education.

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Y1 - 2008/1/1

N2 - 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.

AB - 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.

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KW - Ion channel

KW - K channel blocker

KW - Potassium channel blocker

KW - Sulfonate chalcone

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