About: Toxicity in tumor cells, DNA binding mode, and resistance to decomposition by sulfur nucleophiles of new dinuclear bifunctional trans-Pt-II complexes containing long alkane linkers

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About: Toxicity in tumor cells, DNA binding mode, and resistance to decomposition by sulfur nucleophiles of new dinuclear bifunctional trans-Pt-II complexes containing long alkane linkers Goto Sponge NotDistinct Permalink

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	In an effort to design dinuclear Pt-II compounds that maintain the target (DNA) binding profile of the trans-oriented dinuclear bifunctional Pt-II complexes containing aliphatic linker chains but are less susceptible to metabolic decomposition, the new, long-chain dinuclear Pt-II complexes-[{trans-PtCl(dien)}(2)-mu-(CH2)(n)](2+) (n = 7,10,12, dien = diethylenetriamine)-were synthesized. The toxicity of these metallodrugs was examined in ovarian tumor cell lines. The results showed that the activity of these complexes increased with growing length of the linker; the activity of complex containing the longest linker (n = 12) was comparable with that of cis-diamminedichloridoplatinum(II) (cisplatin). This observation correlated with the results of DNA binding studies performed in cell-free media. The results of these studies demonstrated that the growing length of the aliphatic bridge promoted more distorting conformational alterations induced in DNA. Attention was also paid to the reactivity of {[Pt(dien)Cl](2)-alkane} compounds with glutathione (GSH). In an effort to design dinuclear Pt-II compounds that maintain the target (DNA) binding profile of the trans-oriented dinuclear bifunctional Pt-II complexes containing aliphatic linker chains but are less susceptible to metabolic decomposition, the new, long-chain dinuclear Pt-II complexes-[{trans-PtCl(dien)}(2)-mu-(CH2)(n)](2+) (n = 7,10,12, dien = diethylenetriamine)-were synthesized. The toxicity of these metallodrugs was examined in ovarian tumor cell lines. The results showed that the activity of these complexes increased with growing length of the linker; the activity of complex containing the longest linker (n = 12) was comparable with that of cis-diamminedichloridoplatinum(II) (cisplatin). This observation correlated with the results of DNA binding studies performed in cell-free media. The results of these studies demonstrated that the growing length of the aliphatic bridge promoted more distorting conformational alterations induced in DNA. Attention was also paid to the reactivity of {[Pt(dien)Cl](2)-alkane} compounds with glutathione (GSH). (en)
Title	Toxicity in tumor cells, DNA binding mode, and resistance to decomposition by sulfur nucleophiles of new dinuclear bifunctional trans-Pt-II complexes containing long alkane linkers Toxicity in tumor cells, DNA binding mode, and resistance to decomposition by sulfur nucleophiles of new dinuclear bifunctional trans-Pt-II complexes containing long alkane linkers (en)
skos:prefLabel	Toxicity in tumor cells, DNA binding mode, and resistance to decomposition by sulfur nucleophiles of new dinuclear bifunctional trans-Pt-II complexes containing long alkane linkers Toxicity in tumor cells, DNA binding mode, and resistance to decomposition by sulfur nucleophiles of new dinuclear bifunctional trans-Pt-II complexes containing long alkane linkers (en)
skos:notation	RIV/68081707:_____/13:00392664!RIV14-GA0-68081707
http://linked.open...avai/riv/aktivita	I P S
http://linked.open...avai/riv/aktivity	I, P(GD301/09/H004), S
http://linked.open...iv/cisloPeriodika	2
http://linked.open...vai/riv/dodaniDat	2014
http://linked.open...aciTvurceVysledku	Brabec, Viktor Kašpárková, Jana Nováková, Olga
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Biofyzikální ústav AV ČR, v. v. i.
http://linked.open...dnocenehoVysledku	111419
http://linked.open...ai/riv/idVysledku	RIV/68081707:_____/13:00392664
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	PLATINUM ANTITUMOR COMPLEXES; INTERSTRAND CROSS-LINKS; GEOMETRIC ISOMERISM (en)
http://linked.open.../riv/klicoveSlovo	INTERSTRAND CROSS-LINKS GEOMETRIC ISOMERISM PLATINUM ANTITUMOR COMPLEXES
http://linked.open...odStatuVydavatele	US - Spojené státy americké
http://linked.open...ontrolniKodProRIV	[B181731C1D0E]
http://linked.open...i/riv/nazevZdroje	Pure and Applied Chemistry
http://linked.open...in/vavai/riv/obor	BO
http://linked.open...ichTvurcuVysledku	3 (xsd:int)
http://linked.open...cetTvurcuVysledku	5 (xsd:int)
http://linked.open...vavai/riv/projekt	Molecular and structural biology of selected antitumor drugs. From mechanistic studies to chemotherapy of tumors
http://linked.open...UplatneniVysledku	2013
http://linked.open...v/svazekPeriodika	85
http://linked.open...iv/tvurceVysledku	Brabec, Viktor Kašpárková, Jana Nováková, Olga Gibson, J. Prachařová, J.
http://linked.open...ain/vavai/riv/wos	000314208700004
issn	0033-4545
number of pages	12 (xsd:int)
http://bibframe.org/vocab/doi	10.1351/PAC-CON-12-07-08

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