Discovery of new ATP-competitive inhibitors of human DNA topoisomerase IIα through screening of bacterial topoisomerase inhibitors

[Display omitted] •Discovery of novel chemotype of DNA topoisomerase II inhibitors.•Bacterial topoisomerase inhibitors were an excellent starting point in search of new topo II inhibitors.•The most potent inhibitor had an IC50 of 3.2 µM on topo II.•Two compounds showed very potent activity on MCF-7...

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Veröffentlicht in:	Bioorganic chemistry 2020-09, Vol.102, p.104049-104049, Article 104049
Hauptverfasser:	Skok, Žiga, Durcik, Martina, Gramec Skledar, Darja, Barančoková, Michaela, Peterlin Mašič, Lucija, Tomašič, Tihomir, Zega, Anamarija, Kikelj, Danijel, Zidar, Nace, Ilaš, Janez
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine Triphosphatases - metabolism Anticancer drug Antineoplastic Agents - pharmacology Antineoplastic Agents - therapeutic use ATP-competitive inhibitor Biological screening DNA topoisomerase II DNA Topoisomerases, Type II - chemistry Humans Molecular Docking Simulation N-phenylpyrrolamide Topoisomerase II Inhibitors - pharmacology Topoisomerase II Inhibitors - therapeutic use
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Zusammenfassung:	[Display omitted] •Discovery of novel chemotype of DNA topoisomerase II inhibitors.•Bacterial topoisomerase inhibitors were an excellent starting point in search of new topo II inhibitors.•The most potent inhibitor had an IC50 of 3.2 µM on topo II.•Two compounds showed very potent activity on MCF-7 cell line (IC50
ISSN:	0045-2068 1090-2120
DOI:	10.1016/j.bioorg.2020.104049