Design and characterization of highly in vitro antitumor active ternary copper(II) complexes containing 2'-hydroxychalcone ligands
Jazyk angličtina Země Spojené státy americké Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
27423037
DOI
10.1016/j.jinorgbio.2016.07.005
PII: S0162-0134(16)30199-4
Knihovny.cz E-zdroje
- Klíčová slova
- Antitumor activity, Chalcones, Copper(II), Cytotoxicity, DNA cleavage, In vitro,
- MeSH
- chalkonoidy * chemie farmakologie MeSH
- cytotoxiny * chemická syntéza chemie farmakologie MeSH
- HeLa buňky MeSH
- hepatocyty metabolismus patologie MeSH
- lidé MeSH
- měď * chemie farmakologie MeSH
- MFC-7 buňky MeSH
- nádory farmakoterapie metabolismus patologie MeSH
- protinádorové látky * chemická syntéza chemie farmakologie MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- 2'-hydroxychalcone MeSH Prohlížeč
- chalkonoidy * MeSH
- cytotoxiny * MeSH
- měď * MeSH
- protinádorové látky * MeSH
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.
Citace poskytuje Crossref.org
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