[(p-MeC6H4Pri)2Ru2(SC6H4-p-But)3]Cl (diruthenium-1), a dinuclear arene ruthenium compound with very high anticancer activity: An in vitro and in vivo study

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11150%2F15%3A10283581" target="_blank" >RIV/00216208:11150/15:10283581 - isvavai.cz</a>

Výsledek na webu

<a href="http://www.sciencedirect.com/science/article/pii/S0022328X1400535X" target="_blank" >http://www.sciencedirect.com/science/article/pii/S0022328X1400535X</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.jorganchem.2014.10.050" target="_blank" >10.1016/j.jorganchem.2014.10.050</a>

Jazyk výsledku

angličtina

Název v původním jazyce

[(p-MeC6H4Pri)2Ru2(SC6H4-p-But)3]Cl (diruthenium-1), a dinuclear arene ruthenium compound with very high anticancer activity: An in vitro and in vivo study

Popis výsledku v původním jazyce

A newly synthesised derivative [(p-MeC6H4Pri)2Ru2(SC6H4-p-But)3]Cl (diruthenium-1) with an IC50 value of only 30 nM for both cisplatin-resistant mutant A2780cisR and the normal A2780 cancer cells, was selected for an in vivo anticancer study using a mouse model. In a solid Ehrlcih tumour, diruthenium-1 at doses of 0.4 and 0.6 mg/kg i.p. inhibited the tumour growth, although somewhat less than cisplatin (5 mg/kg i.p.) in the positive control group. However, it was only diruthenium-1 at a dose of 0.6 mg/kg that prolonged significantly the survival rate of the tumour-bearing mice as compared to the untreated control group. A biodistribution study by ICP-MS showed ruthenium to be present in the tumour and particularly in the excretion organs but not in thebrain; the elimination half-life of diruthenium-1 was estimated to be approximately 30 h. In MCF-7 and BT-549 cells, diruthenium-1 exhibited antiproliferative and cytotoxic effects, stimulated the expression and phosphorylation of p53, a

Název v anglickém jazyce

[(p-MeC6H4Pri)2Ru2(SC6H4-p-But)3]Cl (diruthenium-1), a dinuclear arene ruthenium compound with very high anticancer activity: An in vitro and in vivo study

Popis výsledku anglicky

A newly synthesised derivative [(p-MeC6H4Pri)2Ru2(SC6H4-p-But)3]Cl (diruthenium-1) with an IC50 value of only 30 nM for both cisplatin-resistant mutant A2780cisR and the normal A2780 cancer cells, was selected for an in vivo anticancer study using a mouse model. In a solid Ehrlcih tumour, diruthenium-1 at doses of 0.4 and 0.6 mg/kg i.p. inhibited the tumour growth, although somewhat less than cisplatin (5 mg/kg i.p.) in the positive control group. However, it was only diruthenium-1 at a dose of 0.6 mg/kg that prolonged significantly the survival rate of the tumour-bearing mice as compared to the untreated control group. A biodistribution study by ICP-MS showed ruthenium to be present in the tumour and particularly in the excretion organs but not in thebrain; the elimination half-life of diruthenium-1 was estimated to be approximately 30 h. In MCF-7 and BT-549 cells, diruthenium-1 exhibited antiproliferative and cytotoxic effects, stimulated the expression and phosphorylation of p53, a

Druh

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

CEP obor

CE - Biochemie

OECD FORD obor

—

Projekt

—

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 Organometallic Chemistry

ISSN

0022-328X

e-ISSN

—

Svazek periodika

782

Číslo periodika v rámci svazku

April

Stát vydavatele periodika

CH - Švýcarská konfederace

Počet stran výsledku

10

Strana od-do

42-51

Kód UT WoS článku

000351637900008

EID výsledku v databázi Scopus

2-s2.0-84925431451