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Statements

Subject Item
n2:RIV%2F61989592%3A15310%2F08%3A00005500%21RIV10-MSM-15310___
rdf:type
skos:Concept n19:Vysledek
dcterms:description
We have compared the cancer cell cytotoxicity, cell uptake, and DNA binding properties of the isomeric terphenyl complexes [(6-arene)Ru(en)Cl]+, where the arene is ortho- (2), meta- (3), or para-terphenyl (1) (o-, m-, or p-terp). Complex 1, the X-ray crystal structure of which confirms that it has the classical ?piano-stool? geometry, has a similar potency to cisplatin but is not cross-resistant and has a much higher activity than 2 or 3. The extent of Ru uptake into A2780 or A2780cis cells does not correlate with potency. Complex 1 binds to DNA rapidly and quantitatively, preferentially to guanine residues, and causes significant DNA unwinding. Circular and linear dichroism, competitive binding experiments with ethidium bromide, DNA melting, and surface-enhanced Raman spectroscopic data are consistent with combined intercalative and monofunctional (coordination) binding mode of complex 1. This unusual DNA binding mode may therefore make a major contribution to the high potency of complex 1. We have compared the cancer cell cytotoxicity, cell uptake, and DNA binding properties of the isomeric terphenyl complexes [(6-arene)Ru(en)Cl]+, where the arene is ortho- (2), meta- (3), or para-terphenyl (1) (o-, m-, or p-terp). Complex 1, the X-ray crystal structure of which confirms that it has the classical ?piano-stool? geometry, has a similar potency to cisplatin but is not cross-resistant and has a much higher activity than 2 or 3. The extent of Ru uptake into A2780 or A2780cis cells does not correlate with potency. Complex 1 binds to DNA rapidly and quantitatively, preferentially to guanine residues, and causes significant DNA unwinding. Circular and linear dichroism, competitive binding experiments with ethidium bromide, DNA melting, and surface-enhanced Raman spectroscopic data are consistent with combined intercalative and monofunctional (coordination) binding mode of complex 1. This unusual DNA binding mode may therefore make a major contribution to the high potency of complex 1.
dcterms:title
Cytotoxicity, cellular uptake, and DNA interactions of new monodentate ruthenium(II) complexes containing terphenyl arenes Cytotoxicity, cellular uptake, and DNA interactions of new monodentate ruthenium(II) complexes containing terphenyl arenes
skos:prefLabel
Cytotoxicity, cellular uptake, and DNA interactions of new monodentate ruthenium(II) complexes containing terphenyl arenes Cytotoxicity, cellular uptake, and DNA interactions of new monodentate ruthenium(II) complexes containing terphenyl arenes
skos:notation
RIV/61989592:15310/08:00005500!RIV10-MSM-15310___
n3:aktivita
n18:Z n18:P
n3:aktivity
P(1QS500040581), P(GA203/06/1239), P(IAA400040803), P(KAN200200651), P(LC06030), P(ME08017), P(NR8562), P(OC08003), Z(AV0Z50040507), Z(AV0Z50040702), Z(MSM6198959216)
n3:cisloPeriodika
17
n3:dodaniDat
n16:2010
n3:domaciTvurceVysledku
n17:4571932 n17:7988346
n3:druhVysledku
n4:J
n3:duvernostUdaju
n15:S
n3:entitaPredkladatele
n12:predkladatel
n3:idSjednocenehoVysledku
361899
n3:idVysledku
RIV/61989592:15310/08:00005500
n3:jazykVysledku
n6:eng
n3:klicovaSlova
DNA interactions; ruthenium; anticancer
n3:klicoveSlovo
n13:DNA%20interactions n13:ruthenium n13:anticancer
n3:kodStatuVydavatele
US - Spojené státy americké
n3:kontrolniKodProRIV
[C5058A8D90C1]
n3:nazevZdroje
Journal of Medicinal Chemistry
n3:obor
n8:BO
n3:pocetDomacichTvurcuVysledku
2
n3:pocetTvurcuVysledku
10
n3:projekt
n7:LC06030 n7:NR8562 n7:ME08017 n7:IAA400040803 n7:GA203%2F06%2F1239 n7:KAN200200651 n7:1QS500040581 n7:OC08003
n3:rokUplatneniVysledku
n16:2008
n3:svazekPeriodika
51
n3:tvurceVysledku
Brabec, Viktor Kašpárková, Jana Sadler, Peter Pardone, Simon Halámiková, Anna Zerzánková, Lenka Bugarcic, Tijana Habtemariam, Abraha Vrána, Oldřich Nováková, Olga
n3:zamer
n11:MSM6198959216 n11:AV0Z50040507 n11:AV0Z50040702
s:issn
0022-2623
s:numberOfPages
10
n14:organizacniJednotka
15310