title: Synthesis, physico-chemical properties and biological analysis of newly obtained copper(II) complexes with pyrazole derivatives.
abstract: Three new copper(II) complexes containing two different pyrazole bound ligands (1, 2) have been synthesized and characterized by IR, LSI-MS (liquid secondary ion mass spectrometry) and elemental analysis. (1)H NMR spectra of the organic ligands have been recorded. We describe the influence of these complexes on particular cancer cell lines and DNA structure by MTT-assay [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide], APA (acid phosphatase activity)-assay or CD-spectroscopy and agarose gel electrophoresis methods, together with their physico-chemical properties such as lipophilicity and stability in aqueous solution. The cytotoxic effect on HUVEC (endothelial cells) for the most active complex 4 has been also investigated. Moreover, the ability of these complexes to induce apoptosis in cancer cells has been assessed by using fluorescence microscopy. Our results indicate that dichloridobis{1-[amino(thioxo)methyl]-5-hydroxy-3-phenyl-1H-pyrazole-κN2}copper(II) is the most potent complex among the tested complexes.
authors.affiliation: Department of Cosmetic Raw Materials Chemistry, Faculty of Pharmacy, Medical University of Lodz, Muszynski 1 Street, 90-151 Lodz, Poland.
authors.forename: Magdalena
authors.initials: M
authors.lastname: Grazul
authors.affiliation: Institute of Anatomy, University of Zurich, Winterthurerstrasse 190, CH-8057 Zurich, Switzerland.
authors.forename: Emina
authors.initials: E
authors.lastname: Besic-Gyenge
authors.affiliation: Institute of Anatomy, University of Zurich, Winterthurerstrasse 190, CH-8057 Zurich, Switzerland.
authors.forename: Caroline
authors.initials: C
authors.lastname: Maake
authors.affiliation: Department of Cosmetic Raw Materials Chemistry, Faculty of Pharmacy, Medical University of Lodz, Muszynski 1 Street, 90-151 Lodz, Poland.
authors.forename: Michal
authors.initials: M
authors.lastname: Ciolkowski
authors.affiliation: Department of Molecular Biology of Cancer, Medical University of Lodz, Mazowiecka 6/8 Street, 92-215 Lodz, Poland.
authors.forename: Malgorzata
authors.initials: M
authors.lastname: Czyz
authors.affiliation: Institute of Inorganic Chemistry University of Zurich, Winterthurerstrasse 190, CH-8057 Zurich, Switzerland. Electronic address: roland.sigel@aci.uzh.ch.
authors.forename: Roland K O
authors.initials: RK
authors.lastname: Sigel
authors.affiliation: Department of Cosmetic Raw Materials Chemistry, Faculty of Pharmacy, Medical University of Lodz, Muszynski 1 Street, 90-151 Lodz, Poland. Electronic address: elzbieta.budzisz@umed.lodz.pl.
authors.forename: Elzbieta
authors.initials: E
authors.lastname: Budzisz
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D056831:Coordination Complexes / Q000138:chemical synthesis* / Q000494:pharmacology; D003300:Copper / Q000737:chemistry*; D004354:Drug Screening Assays, Antitumor; D004355:Drug Stability; D061307:Human Umbilical Vein Endothelial Cells / Q000187:drug effects / Q000502:physiology; D006801:Humans; D020128:Inhibitory Concentration 50; D011720:Pyrazoles / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D011720:Pyrazoles; D003300:Copper
keywords: Cancer cells; Cytotoxic effect; DNA interactions; Metal(II) complexes; Pyrazole derivative