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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.Vir: European journal of medicinal chemistry. - ISSN 0223-5234 (Vol. 249, 2023, str. 1-21)Vrsta gradiva - članek, sestavni del ; neleposlovje za odrasleLeto - 2023Jezik - angleškiCOBISS.SI-ID - 141491715
Avtor
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
Teme
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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Avtor | Skok, Žiga, farmacevt ... |
Naslov | ATP-competitive inhibitors of human DNA topoisomerase IIα with improved antiproliferative activity based on N-phenylpyrrolamide scaffold |
Datum objave | |
COBISS.SI-ID | 141491715 |
Verzija objave v repozitoriju | Založnikova različica |
Licenca objave v repozitoriju | Creative Commons Priznanje avtorstva 4.0 Mednarodna |
Embargo | Takojšnja javna objava |
Projekti, iz katerih je bila financirana objava
Naziv | Akronim | Številka projekta | Financer |
---|---|---|---|
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 |
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New diagnostic and therapeutic tools against multidrug resistant tumors (STRATAGEM) | 17104 |
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Baze podatkov, v katerih je revija indeksirana
Ime baze podatkov | Področje | Leto |
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Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
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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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