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

Research output: Contribution to journalArticlepeer-review

13 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 languageEnglish
Pages (from-to)12857-12860
Number of pages4
JournalChemical Communications
Volume55
Issue number85
DOIs
StatePublished - 2019

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This journal is © The Royal Society of Chemistry.

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