title: Design and characterization of highly in vitro antitumor active ternary copper(II) complexes containing 2'-hydroxychalcone ligands.
abstract: 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 IC50value 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 IC50value 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.
authors.affiliation: Regional Centre of Advanced Technologies and Materials, Department of Inorganic Chemistry, Faculty of Science, Palacký University in Olomouc, 17. listopadu 12, CZ-771 46 Olomouc, Czech Republic.
authors.forename: Radka
authors.initials: R
authors.lastname: Křikavová
authors.affiliation: Regional Centre of Advanced Technologies and Materials, Department of Inorganic Chemistry, Faculty of Science, Palacký University in Olomouc, 17. listopadu 12, CZ-771 46 Olomouc, Czech Republic.
authors.forename: Ján
authors.initials: J
authors.lastname: Vančo
authors.affiliation: Regional Centre of Advanced Technologies and Materials, Department of Inorganic Chemistry, Faculty of Science, Palacký University in Olomouc, 17. listopadu 12, CZ-771 46 Olomouc, Czech Republic. Electronic address: zdenek.travnicek@upol.cz.
authors.forename: Zdeněk
authors.initials: Z
authors.lastname: Trávníček
authors.affiliation: Regional Centre of Advanced Technologies and Materials, Department of Inorganic Chemistry, Faculty of Science, Palacký University in Olomouc, 17. listopadu 12, CZ-771 46 Olomouc, Czech Republic.
authors.forename: Jakub
authors.initials: J
authors.lastname: Hutyra
authors.affiliation: Regional Centre of Advanced Technologies and Materials, Department of Cell Biology and Genetics, Faculty of Science, Palacký University in Olomouc, Šlechtitelů 27, CZ-783 71 Olomouc, Czech Republic.
authors.forename: Zdeněk
authors.initials: Z
authors.lastname: Dvořák
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D047188:Chalcones / Q000737:chemistry / Q000494:pharmacology; D003300:Copper / Q000737:chemistry / Q000494:pharmacology; D003603:Cytotoxins / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006367:HeLa Cells; D022781:Hepatocytes / Q000378:metabolism / Q000473:pathology; D006801:Humans; D061986:MCF-7 Cells; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology
chemical_list: D000970:Antineoplastic Agents; D047188:Chalcones; D003603:Cytotoxins; D003300:Copper; C013031:2'-hydroxychalcone
keywords: Antitumor activity; Chalcones; Copper(II); Cytotoxicity; DNA cleavage; In vitro