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ATP-competitive inhibitors of human DNA topoisomerase IIα with improved antiproliferative activity based on N-phenylpyrrolamide scaffoldSkok, Žiga, farmacevt ...ATP-competitive inhibitors of human DNA topoisomerase II show potential for becoming the successors of topoisomerase II poisons, the clinically successful anticancer drugs. Based on our recent ... screening hits, we designed, synthesized and biologically evaluated new, improved series of N-phenylpyrrolamide DNA topoisomerase II inhibitors. Six structural classes were prepared to systematically explore the chemical space of N-phenylpyrrolamide based inhibitors. The most potent inhibitor, 47d, had an IC50 value of 0.67 μM against DNA topoisomerase IIα. Compound 53b showed exceptional activity on cancer cell lines with IC50 values of 130 nM against HepG2 and 140 nM against MCF-7 cancer cell lines. The reported compounds have no structurally similarity to published structures, they are metabolically stable, have reasonable solubility and thus can serve as promising leads in the development of anticancer ATP-competitive inhibitors of human DNA topoisomerase IIα.Source: European journal of medicinal chemistry. - ISSN 0223-5234 (Vol. 249, 2023, str. 1-21)Type of material - article, component part ; adult, seriousPublish date - 2023Language - englishCOBISS.SI-ID - 141491715
Author
Skok, Žiga, farmacevt |
Durcik, Martina |
Zajec, Živa, farmacevtka |
Gramec, Darja, farmacevtka |
Bozovičar, Krištof |
Pišlar, Anja |
Tomašič, Tihomir |
Zega, Anamarija |
Peterlin-Mašič, Lucija |
Kikelj, Danijel |
Zidar, Nace |
Ilaš, Janez
Topics
Rak (medicina) |
Farmacevtska kemija |
Citotoksičnost |
ATP-kompetitivni katalitični zaviralec |
človeška DNA topoizomeraza II |
anticancer |
ATP-competitive |
Catalytic inhibitor |
cytotoxic |
human DNA topoisomerase II
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Author | Skok, Žiga, farmacevt ... |
Title | ATP-competitive inhibitors of human DNA topoisomerase IIα with improved antiproliferative activity based on N-phenylpyrrolamide scaffold |
Publication date | |
COBISS.SI-ID | 141491715 |
Publication version in repository | Publisher's version |
Publication licence | Creative Commons Attribution 4.0 International |
Embargo | Immediate publication for public |
Project(s) from which the publication was funded
Title | Acronym | Project ID | Funder |
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Farmacevtska kemija: načrtovanje, sinteza in vrednotenje učinkovin | P1-0208-2022 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
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Fotokemijski pristop za odkrivanje naprednih ATP-kompetitivnih prob z zaviralnim delovanjem na Topoizomerazo IIalfa | N1-0172-2021 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
|
New diagnostic and therapeutic tools against multidrug resistant tumors (STRATAGEM) | 17104 |
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Skok, Žiga, farmacevt | 39202 |
Durcik, Martina | 50490 |
Zajec, Živa, farmacevtka | 53670 |
Gramec, Darja, farmacevtka | 35432 |
Bozovičar, Krištof | 53738 |
Pišlar, Anja | 32035 |
Tomašič, Tihomir | 28334 |
Zega, Anamarija | 18633 |
Peterlin-Mašič, Lucija | 19317 |
Kikelj, Danijel | 01463 |
Zidar, Nace | 28905 |
Ilaš, Janez | 24400 |
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