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

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

Seojeong Park,‡^a Soo-Yeon Hwang,‡^a Jaeho Shin,^b Hyunji Jo,^a Younghwa Na*^b and Youngjoo Kwon

*^a

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* Corresponding authors

^a College of Pharmacy & Graduate School of Pharmaceutical Sciences, Ewha Womans University, Seoul, Korea
E-mail: ykwon@ewha.ac.kr

^b College of Pharmacy, CHA University, Pocheon, Korea
E-mail: yna7315@cha.ac.kr

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.

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Article information

DOI: https://doi.org/10.1039/C9CC05524J
Article type: Communication
Submitted: 17 Jul 2019
Accepted: 25 Sep 2019
First published: 02 Oct 2019

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Chem. Commun., 2019,55, 12857-12860

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

S. Park, S. Hwang, J. Shin, H. Jo, Y. Na and Y. Kwon, Chem. Commun., 2019, 55, 12857 DOI: 10.1039/C9CC05524J

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Chemical Communications

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

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