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

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F68081707%3A_____%2F15%3A00442212" target="_blank" >RIV/68081707:_____/15:00442212 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/61989592:15310/15:33155835

Výsledek na webu

<a href="http://dx.doi.org/10.1021/jm501420k" target="_blank" >http://dx.doi.org/10.1021/jm501420k</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1021/jm501420k" target="_blank" >10.1021/jm501420k</a>

Jazyk výsledku

angličtina

Název v původním jazyce

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

Popis výsledku v původním jazyce

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 aswell 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 roleof 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 a

Název v anglickém jazyce

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

Popis výsledku anglicky

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 aswell 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 roleof 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 a

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

BO - Biofyzika

OECD FORD obor

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Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2015

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Journal of Medicinal Chemistry

ISSN

0022-2623

e-ISSN

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Svazek periodika

58

Číslo periodika v rámci svazku

2

Stát vydavatele periodika

US - Spojené státy americké

Počet stran výsledku

13

Strana od-do

847-859

Kód UT WoS článku

000348492100025

EID výsledku v databázi Scopus

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