A chromenone analog as an ATP-competitive, DNA non-intercalative topoisomerase II catalytic inhibitor with preferences toward the alpha isoform

Seojeong Park; Soo Yeon Hwang; Jaeho Shin; Hyunji Jo; Younghwa Na; Youngjoo Kwon

doi:10.1039/c9cc05524j

A chromenone analog as an ATP-competitive, DNA non-intercalative topoisomerase II catalytic inhibitor with preferences toward the alpha isoform

Seojeong Park
, Soo Yeon Hwang
, Jaeho Shin
, Hyunji Jo
, Younghwa Na
, Youngjoo Kwon

Department of Pharmaceutical Sciences

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

14 Scopus citations

Abstract

5-Hydroxy-2-phenyl-7-(thiiran-2-ylmethoxy)-4H-chromen-4-one (compound 52) was found as a DNA non-intercalative topo II specific catalytic inhibitor by targeting its ATP-binding domain. Showing changes in interaction with Mg²⁺, it exhibited highly selective properties against the α-isoform with less toxicity, unlike other topo II poisons, such as etoposide.

Original language	English
Pages (from-to)	12857-12860
Number of pages	4
Journal	Chemical Communications
Volume	55
Issue number	85
DOIs	https://doi.org/10.1039/c9cc05524j
State	Published - 2019

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Publisher Copyright:
This journal is © The Royal Society of Chemistry.

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title = "A chromenone analog as an ATP-competitive, DNA non-intercalative topoisomerase II catalytic inhibitor with preferences toward the alpha isoform",

abstract = "5-Hydroxy-2-phenyl-7-(thiiran-2-ylmethoxy)-4H-chromen-4-one (compound 52) was found as a DNA non-intercalative topo II specific catalytic inhibitor by targeting its ATP-binding domain. Showing changes in interaction with Mg2+, it exhibited highly selective properties against the α-isoform with less toxicity, unlike other topo II poisons, such as etoposide.",

author = "Seojeong Park and Hwang, \{Soo Yeon\} and Jaeho Shin and Hyunji Jo and Younghwa Na and Youngjoo Kwon",

note = "Publisher Copyright: This journal is {\textcopyright} The Royal Society of Chemistry.",

year = "2019",

doi = "10.1039/c9cc05524j",

language = "English",

volume = "55",

pages = "12857--12860",

journal = "Chemical Communications",

issn = "1359-7345",

publisher = "Royal Society of Chemistry",

number = "85",

}

TY - JOUR

T1 - A chromenone analog as an ATP-competitive, DNA non-intercalative topoisomerase II catalytic inhibitor with preferences toward the alpha isoform

AU - Park, Seojeong

AU - Hwang, Soo Yeon

AU - Shin, Jaeho

AU - Jo, Hyunji

AU - Na, Younghwa

AU - Kwon, Youngjoo

N1 - Publisher Copyright: This journal is © The Royal Society of Chemistry.

PY - 2019

Y1 - 2019

N2 - 5-Hydroxy-2-phenyl-7-(thiiran-2-ylmethoxy)-4H-chromen-4-one (compound 52) was found as a DNA non-intercalative topo II specific catalytic inhibitor by targeting its ATP-binding domain. Showing changes in interaction with Mg2+, it exhibited highly selective properties against the α-isoform with less toxicity, unlike other topo II poisons, such as etoposide.

AB - 5-Hydroxy-2-phenyl-7-(thiiran-2-ylmethoxy)-4H-chromen-4-one (compound 52) was found as a DNA non-intercalative topo II specific catalytic inhibitor by targeting its ATP-binding domain. Showing changes in interaction with Mg2+, it exhibited highly selective properties against the α-isoform with less toxicity, unlike other topo II poisons, such as etoposide.

UR - https://www.scopus.com/pages/publications/85073665101

U2 - 10.1039/c9cc05524j

DO - 10.1039/c9cc05524j

M3 - Article

C2 - 31598611

AN - SCOPUS:85073665101

SN - 1359-7345

VL - 55

SP - 12857

EP - 12860

JO - Chemical Communications

JF - Chemical Communications

IS - 85

ER -

A chromenone analog as an ATP-competitive, DNA non-intercalative topoisomerase II catalytic inhibitor with preferences toward the alpha isoform

Abstract

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