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- W1979555212 abstract "A series of organoruthenium(II) chlorido complexes with fluorinated O,O-ligands [(η6-p-cymene)Ru(F3C-acac-Ar)Cl] (1a–6a) and their respective 1,3,5-triaza-7-phosphaadamantane (pta) derivatives [(η6-p-cymene)Ru(F3C-acac-Ar)pta]PF6 (1b–6b) were synthesized and fully characterized in both solution and solid state. All complexes were inactive against nonmalignant keratinocytes but displayed variable activity against cancer cell models (ovarian, osteosarcoma). Compounds with a ligand containing the 4-chlorophenyl substituent (6a and 6b) exhibited the strongest anticancer effects. Despite a marginally lower cellular Ru accumulation compared to the chlorido complexes, pta analogues showed higher activity especially in the osteosarcoma model. Reduction of glutathione levels by buthionine sulfoximine (BSO) significantly enhanced the activity of all compounds with the most pronounced effects being observed for the pta series resulting in IC50 values down to the nanomolar range. While all chlorido complexes potently induce reactive oxygen species, DNA damage, and apoptosis, the respective pta compounds widely lacked ROS production but blocked cell cycle progression in G0/G1 phase." @default.
- W1979555212 created "2016-06-24" @default.
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- W1979555212 date "2015-04-17" @default.
- W1979555212 modified "2023-10-07" @default.
- W1979555212 title "Structure-Related Mode-of-Action Differences of Anticancer Organoruthenium Complexes with β-Diketonates" @default.
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- W1979555212 doi "https://doi.org/10.1021/acs.jmedchem.5b00288" @default.
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