Biological Activity of Triazolopyrimidine Copper(II) Complexes Modulated by an Auxiliary N-N-Chelating Heterocycle Ligands
Lavinia L. Ruta,
Ileana C. Farcasanu,
Mihaela Bacalum,
Mina Răileanu,
Arpad Mihai Rostas,
Constantin Daniliuc,
Mariana Carmen Chifiriuc,
Luminița Măruțescu,
Marcela Popa,
Mihaela Badea,
Emilia Elena Iorgulescu,
Rodica Olar
Affiliations
Lavinia L. Ruta
Department of Organic Chemistry, Biochemistry and Catalysis, Faculty of Chemistry, University of Bucharest, 90–92 Panduri Str., 050663 Bucharest, Romania
Ileana C. Farcasanu
Department of Organic Chemistry, Biochemistry and Catalysis, Faculty of Chemistry, University of Bucharest, 90–92 Panduri Str., 050663 Bucharest, Romania
Mihaela Bacalum
Department of Life and Environmental Physics, Horia Hulubei National Institute for Physics and Nuclear Engineering, 30 Reactorului Str., 077125 Măgurele, Romania
Mina Răileanu
Department of Life and Environmental Physics, Horia Hulubei National Institute for Physics and Nuclear Engineering, 30 Reactorului Str., 077125 Măgurele, Romania
Arpad Mihai Rostas
Laboratory of Atomic Structures and Defects in Advanced Materials, National Institute of Materials Physics, 405A Atomiştilor Str., 077125 Măgurele, Romania
Constantin Daniliuc
Organisch-Chemisches Institute, Westfälische Wilhelms-Universität Münster, Corrensstrasse 40, 48149 Münster, Germany
Mariana Carmen Chifiriuc
Department of Microbiology, Faculty of Biology, University of Bucharest, 1–3 Aleea Portocalelor Str., 060101 Bucharest, Romania
Luminița Măruțescu
Department of Microbiology, Faculty of Biology, University of Bucharest, 1–3 Aleea Portocalelor Str., 060101 Bucharest, Romania
Marcela Popa
Department of Microbiology, Faculty of Biology, University of Bucharest, 1–3 Aleea Portocalelor Str., 060101 Bucharest, Romania
Mihaela Badea
Department of Inorganic Chemistry, Biochemistry and Catalysis, Faculty of Chemistry, University of Bucharest, 90–92 Panduri Str., 050663 Bucharest, Romania
Emilia Elena Iorgulescu
Department of Analytical Chemistry, Faculty of Chemistry, University of Bucharest, 90–92 Panduri Str., 050663 Bucharest, Romania
Rodica Olar
Department of Inorganic Chemistry, Biochemistry and Catalysis, Faculty of Chemistry, University of Bucharest, 90–92 Panduri Str., 050663 Bucharest, Romania
Novel complexes of type [Cu(N-N)(dmtp)2(OH2)](ClO4)2·dmtp ((1) N-N: 2,2′-bipyridine; (2) L: 1,10-phenantroline and dmtp: 5,7-dimethyl-1,2,4-triazolo[1,5-a]pyrimidine) were designed in order to obtain biologically active compounds. Complexes were characterized as mononuclear species that crystallized in the space group P-1 of the triclinic system with a square pyramidal geometry around the copper (II). In addition to the antiproliferative effect on murine melanoma B16 cells, complex (1) exhibited low toxicity on normal BJ cells and did not affect membrane integrity. Complex (2) proved to be a more potent antimicrobial in comparison with (1), but both compounds were more active in comparison with dmtp—both against planktonic cells and biofilms. A stronger antimicrobial and antibiofilm effect was noticed against the Gram-positive strains, including methicillin-resistant Staphylococcus aureus (MRSA). Both electron paramagnetic resonance (EPR) and Saccharomyces cerevisiae studies indicated that the complexes were scavengers rather than reactive oxygen species promoters. Their DNA intercalating capacity was evidenced by modifications in both absorption and fluorescence spectra. Furthermore, both complexes exhibited nuclease-like activity, which increased in the presence of hydrogen peroxide.
