| Attributes | Values |
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| rdf:type
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| Description
| - The effect of replacement of the N,N-chelating ligand 1,10-phenanthroline (phen) in the Ir-III pentamethylcyclopentadienyl (Cp-star) complex [(eta(5)-Cp-star)(Ir)(phen) Cl](+) (2) with the C,N-chelating ligand 7,8-benzoquinoline (bq) to give [(eta(5)-Cp-star)(Ir)(bq)Cl] (1) on the cytotoxicity of these (CpIrIII)-Ir-star complexes toward cancer cell lines was investigated. Complex 2 is inactive, similar to other (CpIrIII)-Ir-star complexes containing the N, N-chelating ligands. In contrast, a single atom change (C- for N) in the chelating N, N ligand resulted in potency in human ovarian carcinoma cisplatin-sensitive A2780 cells, and, strikingly, 1 is active in the cisplatin-resistant human breast cancer MCF-7 and A2780/cisR cells. Replacement of the N,N-chelating ligand with the C,N-chelating ligand gives rise to increased hydrophobicity, leading to higher cellular accumulation, higher DNA-bound iridium in cells and higher cytotoxicity. The pathways involved in cellular accumulation of 1 have been further explored and compared with conventional cisplatin. The results show that both energy-independent passive diffusion and energy-dependent transport play a role in accumulation of 1.
- The effect of replacement of the N,N-chelating ligand 1,10-phenanthroline (phen) in the Ir-III pentamethylcyclopentadienyl (Cp-star) complex [(eta(5)-Cp-star)(Ir)(phen) Cl](+) (2) with the C,N-chelating ligand 7,8-benzoquinoline (bq) to give [(eta(5)-Cp-star)(Ir)(bq)Cl] (1) on the cytotoxicity of these (CpIrIII)-Ir-star complexes toward cancer cell lines was investigated. Complex 2 is inactive, similar to other (CpIrIII)-Ir-star complexes containing the N, N-chelating ligands. In contrast, a single atom change (C- for N) in the chelating N, N ligand resulted in potency in human ovarian carcinoma cisplatin-sensitive A2780 cells, and, strikingly, 1 is active in the cisplatin-resistant human breast cancer MCF-7 and A2780/cisR cells. Replacement of the N,N-chelating ligand with the C,N-chelating ligand gives rise to increased hydrophobicity, leading to higher cellular accumulation, higher DNA-bound iridium in cells and higher cytotoxicity. The pathways involved in cellular accumulation of 1 have been further explored and compared with conventional cisplatin. The results show that both energy-independent passive diffusion and energy-dependent transport play a role in accumulation of 1. (en)
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| Title
| - Mechanism of cellular accumulation of an iridium(III) pentamethylcyclopentadienyl anticancer complex containing a C,N-chelating ligand
- Mechanism of cellular accumulation of an iridium(III) pentamethylcyclopentadienyl anticancer complex containing a C,N-chelating ligand (en)
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| skos:prefLabel
| - Mechanism of cellular accumulation of an iridium(III) pentamethylcyclopentadienyl anticancer complex containing a C,N-chelating ligand
- Mechanism of cellular accumulation of an iridium(III) pentamethylcyclopentadienyl anticancer complex containing a C,N-chelating ligand (en)
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| skos:notation
| - RIV/68081707:_____/14:00428115!RIV15-AV0-68081707
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| http://linked.open...avai/riv/aktivita
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| http://linked.open...avai/riv/aktivity
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| http://linked.open...iv/cisloPeriodika
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| http://linked.open...vai/riv/dodaniDat
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| http://linked.open...aciTvurceVysledku
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| http://linked.open.../riv/druhVysledku
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| http://linked.open...iv/duvernostUdaju
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| http://linked.open...titaPredkladatele
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| http://linked.open...dnocenehoVysledku
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| http://linked.open...ai/riv/idVysledku
| - RIV/68081707:_____/14:00428115
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| http://linked.open...riv/jazykVysledku
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| http://linked.open.../riv/klicovaSlova
| - HUMAN OVARIAN-CANCER; DRUG-RESISTANCE; P-GLYCOPROTEIN (en)
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| http://linked.open.../riv/klicoveSlovo
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| http://linked.open...odStatuVydavatele
| - GB - Spojené království Velké Británie a Severního Irska
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| http://linked.open...ontrolniKodProRIV
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| http://linked.open...i/riv/nazevZdroje
| |
| http://linked.open...in/vavai/riv/obor
| |
| http://linked.open...ichTvurcuVysledku
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| http://linked.open...cetTvurcuVysledku
| |
| http://linked.open...vavai/riv/projekt
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| http://linked.open...UplatneniVysledku
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| http://linked.open...v/svazekPeriodika
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| http://linked.open...iv/tvurceVysledku
| - Brabec, Viktor
- Kašpárková, Jana
- Sadler, P. J.
- Vojtíšková, Marie
- Novohradský, Vojtěch
- Liu, Z.
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| http://linked.open...ain/vavai/riv/wos
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| issn
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| number of pages
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| http://bibframe.org/vocab/doi
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