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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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Publication details

The article was received on 17 Jul 2019, accepted on 25 Sep 2019 and first published on 02 Oct 2019


Article type: Communication
DOI: 10.1039/C9CC05524J
Chem. Commun., 2019, Advance Article

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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, Advance Article , DOI: 10.1039/C9CC05524J

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