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Ruthenium complexes show potent inhibition of AKR1C1, AKR1C2, and AKR1C3 enzymes and anti-proliferative action against chemoresistant ovarian cancer cell line [Elektronski vir]Kljun, Jakob ...In this study, we present the synthesis, kinetic studies of inhibitory activity toward aldo-keto reductase 1C (AKR1C) enzymes, and anticancer potential toward chemoresistant ovarian cancer of 10 ... organoruthenium compounds bearing diketonate (1–6) and hydroxyquinolinate (7–10) chelating ligands with the general formula [(η6-p-cymene)Ru (chel) (X)]n+ where chel represents the chelating ligand and X the chlorido or pta ligand. Our studies show that these compounds are potent inhibitors of the AKR enzymes with an uncommon inhibitory mechanism, where two inhibitor molecules bind to the enzyme in a first fast and reversible step and a second slower and irreversible step. The binding potency of each step is dependent on the chemical structure of the monodentate ligands in the metalloinhibitors with the chlorido complexes generally acting as reversible inhibitors and pta complexes as irreversible inhibitors. Our study also shows that compounds 1–9 have a moderate yet better anti-proliferative and anti-migration action on the chemoresistant ovarian cancer cell line COV362 compared to carboplatin and similar effects to cisplatin.Source: Frontiers in pharmacology [Elektronski vir]. - ISSN 1663-9812 (Vol. 13, Aug. 2022, str. 1-15)Type of material - e-article ; adult, seriousPublish date - 2022Language - englishCOBISS.SI-ID - 115794691
Author
Kljun, Jakob |
Pavlič, Renata |
Hafner, Eva, 1987- |
Lipec, Tanja |
Moreno-Da Silva, Sara |
Tič, Primož |
Turel, Iztok |
Büdefeld, Tomaž |
Stojan, Jure, 1956- |
Lanišnik-Rižner, Tea
Topics
ruthenium complexes |
synthesis |
crystal structure |
rutenijevi kompleksi |
sinteza |
kristalna struktura
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DRS, in which the journal is indexed
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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Kljun, Jakob | 30698 |
Pavlič, Renata | 38391 |
Hafner, Eva, 1987- | 53995 |
Lipec, Tanja | ![]() |
Moreno-Da Silva, Sara | ![]() |
Tič, Primož | ![]() |
Turel, Iztok | 11053 |
Büdefeld, Tomaž | 29835 |
Stojan, Jure, 1956- | 03723 |
Lanišnik-Rižner, Tea | 11699 |
Source: Personal bibliographies
and: SICRIS
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