About: Novel Antitumor Cisplatin and Transplatin Derivatives Containing 1-Methyl-7-Azaindole: Synthesis, Characterization, and Cellular Responses

Facets (new session)
Description
Metadata
Settings
- owl:sameAs
- Inference Rule:

About: Novel Antitumor Cisplatin and Transplatin Derivatives Containing 1-Methyl-7-Azaindole: Synthesis, Characterization, and Cellular Responses Goto Sponge NotDistinct Permalink

An Entity of Type : http://linked.opendata.cz/ontology/domain/vavai/Vysledek, within Data Space : linked.opendata.cz associated with source document(s)

Attributes	Values
rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	The current work investigates the effect of new bifunctional and mononuclear Pt(II) compounds, the cis- and trans-isomers of [PtCl2(NH3)(L)] (L = 1-methyl-7-azaindole, compounds 1 and 2, respectively), on growth and viability of human carcinoma cells as well as their putative mechanism(s) of cytotoxicity. The results show that substitution of 1-methyl-7-azaindole for ammine in cisplatin or transplatin results in an increase of the toxic efficiency, selectivity for tumor cells in cisplatin-resistant cancer cells, and activation of the trans geometry. The differences in the cytotoxic activities of 1 and 2 were suggested to be due to their different DNA binding mode, different capability to induce cell cycle perturbations, and fundamentally different role of transcription factor p53 in their mechanism of action. Interestingly, both isomers make it possible to detect their cellular uptake and distribution in living cells by confocal microscopy without their modification with an optically active tag. The current work investigates the effect of new bifunctional and mononuclear Pt(II) compounds, the cis- and trans-isomers of [PtCl2(NH3)(L)] (L = 1-methyl-7-azaindole, compounds 1 and 2, respectively), on growth and viability of human carcinoma cells as well as their putative mechanism(s) of cytotoxicity. The results show that substitution of 1-methyl-7-azaindole for ammine in cisplatin or transplatin results in an increase of the toxic efficiency, selectivity for tumor cells in cisplatin-resistant cancer cells, and activation of the trans geometry. The differences in the cytotoxic activities of 1 and 2 were suggested to be due to their different DNA binding mode, different capability to induce cell cycle perturbations, and fundamentally different role of transcription factor p53 in their mechanism of action. Interestingly, both isomers make it possible to detect their cellular uptake and distribution in living cells by confocal microscopy without their modification with an optically active tag. (en)
Title	Novel Antitumor Cisplatin and Transplatin Derivatives Containing 1-Methyl-7-Azaindole: Synthesis, Characterization, and Cellular Responses Novel Antitumor Cisplatin and Transplatin Derivatives Containing 1-Methyl-7-Azaindole: Synthesis, Characterization, and Cellular Responses (en)
skos:prefLabel	Novel Antitumor Cisplatin and Transplatin Derivatives Containing 1-Methyl-7-Azaindole: Synthesis, Characterization, and Cellular Responses Novel Antitumor Cisplatin and Transplatin Derivatives Containing 1-Methyl-7-Azaindole: Synthesis, Characterization, and Cellular Responses (en)
skos:notation	RIV/68081707:_____/15:00442212!RIV15-AV0-68081707
http://linked.open...avai/riv/aktivita	I P
http://linked.open...avai/riv/aktivity	I, P(LD14019)
http://linked.open...iv/cisloPeriodika	2
http://linked.open...vai/riv/dodaniDat	2015
http://linked.open...aciTvurceVysledku	Brabec, Viktor Kašpárková, Jana Nováková, Olga Novohradský, Vojtěch
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	320
http://linked.open...ai/riv/idVysledku	RIV/68081707:_____/15:00442212
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	INTERSTRAND CROSS-LINKS; PLATINUM(II) COMPLEXES; TUMOR-CELLS (en)
http://linked.open.../riv/klicoveSlovo	INTERSTRAND CROSS-LINKS TUMOR-CELLS PLATINUM(II) COMPLEXES
http://linked.open...odStatuVydavatele	US - Spojené státy americké
http://linked.open...ontrolniKodProRIV	[9803E89187E6]
http://linked.open...i/riv/nazevZdroje	Journal of Medicinal Chemistry
http://linked.open...in/vavai/riv/obor	BO
http://linked.open...ichTvurcuVysledku	4 (xsd:int)
http://linked.open...cetTvurcuVysledku	12 (xsd:int)
http://linked.open...vavai/riv/projekt	Molekulární a buněčná farmakologie nových konjugovaných organokovových sloučenin. Vztah k vývoji nových léčiv proti rakovině.
http://linked.open...UplatneniVysledku	2015
http://linked.open...v/svazekPeriodika	58
http://linked.open...iv/tvurceVysledku	Brabec, Viktor Kašpárková, Jana Nováková, Olga Muchová, T. Novohradský, Vojtěch Natile, G. Prachařová, J. Ilík, P. Intini, F. P. Pacifico, C. Saltarella, T. Scintilla, S.
http://linked.open...ain/vavai/riv/wos	000348492100025
issn	0022-2623
number of pages	13 (xsd:int)
http://bibframe.org/vocab/doi	10.1021/jm501420k

Faceted Search & Find service v1.16.118 as of Jun 21 2024

Alternative Linked Data Documents: ODE Content Formats:

RDF

ODATA

Microdata

About

OpenLink Virtuoso version 07.20.3240 as of Jun 21 2024, on Linux (x86_64-pc-linux-gnu), Single-Server Edition (126 GB total memory, 58 GB memory in use)
Data on this page belongs to its respective rights holders.
Virtuoso Faceted Browser Copyright © 2009-2024 OpenLink Software