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

Result code in 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>
Result on the web
<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>

Result language
angličtina
Original language name
Design and characterization of highly in vitro antitumor active ternary copper(II) complexes containing 2'-hydroxychalcone ligands
Original language description
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.
Czech name
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Czech description
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Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
FR - Pharmacology and apothecary chemistry
OECD FORD branch
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Project
<a href="/en/project/LO1305" target="_blank" >LO1305: Development of the center of advanced technologies and materials</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>S - Specificky vyzkum na vysokych skolach

Publication year
2016
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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