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Issue 85, 2019
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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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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.

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

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Article information


Submitted
17 Jul 2019
Accepted
25 Sep 2019
First published
02 Oct 2019

Chem. Commun., 2019,55, 12857-12860
Article type
Communication

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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