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Statements

Subject Item
n2:RIV%2F68081707%3A_____%2F14%3A00428115%21RIV15-AV0-68081707
rdf:type
skos:Concept n15:Vysledek
dcterms: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.
dcterms: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
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
skos:notation
RIV/68081707:_____/14:00428115!RIV15-AV0-68081707
n3:aktivita
n11:S n11:P n11:I
n3:aktivity
I, P(EE2.3.20.0057), S
n3:cisloPeriodika
3
n3:dodaniDat
n14:2015
n3:domaciTvurceVysledku
n9:4571932 n9:1966154 n9:7988346 n9:6854974
n3:druhVysledku
n10:J
n3:duvernostUdaju
n6:S
n3:entitaPredkladatele
n16:predkladatel
n3:idSjednocenehoVysledku
28125
n3:idVysledku
RIV/68081707:_____/14:00428115
n3:jazykVysledku
n13:eng
n3:klicovaSlova
HUMAN OVARIAN-CANCER; DRUG-RESISTANCE; P-GLYCOPROTEIN
n3:klicoveSlovo
n5:P-GLYCOPROTEIN n5:DRUG-RESISTANCE n5:HUMAN%20OVARIAN-CANCER
n3:kodStatuVydavatele
GB - Spojené království Velké Británie a Severního Irska
n3:kontrolniKodProRIV
[289F1CE37EEF]
n3:nazevZdroje
Metallomics
n3:obor
n8:BO
n3:pocetDomacichTvurcuVysledku
4
n3:pocetTvurcuVysledku
6
n3:projekt
n18:EE2.3.20.0057
n3:rokUplatneniVysledku
n14:2014
n3:svazekPeriodika
6
n3:tvurceVysledku
Novohradský, Vojtěch Vojtíšková, Marie Liu, Z. Brabec, Viktor Sadler, P. J. Kašpárková, Jana
n3:wos
000333565800030
s:issn
1756-5901
s:numberOfPages
9
n17:doi
10.1039/c3mt00341h