Design and characterization of highly in vitro antitumor active ternary copper(II) complexes containing 2'-hydroxychalcone ligands

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F16%3A33159498" target="_blank" >RIV/61989592:15310/16:33159498 - isvavai.cz</a>

Výsledek na webu

<a href="http://www.sciencedirect.com/science/article/pii/S0162013416301994" target="_blank" >http://www.sciencedirect.com/science/article/pii/S0162013416301994</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.jinorgbio.2016.07.005" target="_blank" >10.1016/j.jinorgbio.2016.07.005</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Design and characterization of highly in vitro antitumor active ternary copper(II) complexes containing 2'-hydroxychalcone ligands

Popis výsledku v původním jazyce

A series of innovative copper(II) complexes of the general composition [Cu(Ln)(phen)]NO3 (1-8; phen=1,10-phenanthroline), involving 2'-hydroxychalcone {(E)-1-(2'-hydroxyphenyl)-3-phenylprop-2-en-1-one} derivatives (HLn) was synthesized, thoroughly characterized and screened for in vitro cytotoxicity against a panel of ten human cancer cell lines. The most promising results were achieved for complex 2 with the best IC50 value of 1.1+-0.7μM (against A2780 cell line). The toxicity testing on a primary culture of human hepatocytes (HH) revealed that complex 2 is the least toxic from the whole series with the IC50 value of 63.7μM. The complexes were shown to be able to efficaciously cleave pUC19 plasmid DNA as well as intercalate into calf thymus DNA with the same affinity and efficacy as ethidium bromide and interact by the ligand exchange mechanism with l-cysteine at physiological concentration levels.

Název v anglickém jazyce

Design and characterization of highly in vitro antitumor active ternary copper(II) complexes containing 2'-hydroxychalcone ligands

Popis výsledku anglicky

A series of innovative copper(II) complexes of the general composition [Cu(Ln)(phen)]NO3 (1-8; phen=1,10-phenanthroline), involving 2'-hydroxychalcone {(E)-1-(2'-hydroxyphenyl)-3-phenylprop-2-en-1-one} derivatives (HLn) was synthesized, thoroughly characterized and screened for in vitro cytotoxicity against a panel of ten human cancer cell lines. The most promising results were achieved for complex 2 with the best IC50 value of 1.1+-0.7μM (against A2780 cell line). The toxicity testing on a primary culture of human hepatocytes (HH) revealed that complex 2 is the least toxic from the whole series with the IC50 value of 63.7μM. The complexes were shown to be able to efficaciously cleave pUC19 plasmid DNA as well as intercalate into calf thymus DNA with the same affinity and efficacy as ethidium bromide and interact by the ligand exchange mechanism with l-cysteine at physiological concentration levels.

Druh

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

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

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Projekt

<a href="/cs/project/LO1305" target="_blank" >LO1305: Rozvoj centra pokročilých technologií a materiálů</a><br>

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>S - Specificky vyzkum na vysokych skolach

Rok uplatnění

2016

Kód důvěrnosti údajů

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

Název periodika

Journal of Inorganic Biochemistry

ISSN

0162-0134

e-ISSN

—

Svazek periodika

163

Číslo periodika v rámci svazku

OCT

Stát vydavatele periodika

US - Spojené státy americké

Počet stran výsledku

10

Strana od-do

8-17

Kód UT WoS článku

000388546800002

EID výsledku v databázi Scopus

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