title: Synthesis and characterization of some new complexes of Cu(II), Ni(II) and V(IV) with Schiff base derived from indole-3-carboxaldehyde. Biological activity on prokaryotes and eukaryotes.
abstract: Six new Cu(II), Ni(II), and VO(II) complexes (1-6) with Schiff base 1-phenyl-2,3-dimethyl-4-(1H-indole-3-carboxaldehyde)-3-pyrazolin-5-one (HL) were synthesized. The Schiff base was prepared through the condensation of 1-phenyl-2,3-dimethyl-4-amino-3-pyrazolin-5-one (antipyrine) with 1H-indole-3-carboxaldehyde. The new obtained compounds were characterized by (1)H NMR, (13)C NMR, UV-VIS, IR, EPR spectroscopy, elemental analysis, molar electric conductibility, magnetic susceptibility and thermal gravimetric analysis. In addition, the structure of the ligand HL has been determined by X-ray diffraction methods. The biological activity of complex compounds was investigated in terms of antibacterial effect on prokaryotic cells, by using paper disc diffusion technique, and for antiproliferative effect on eukaryotic cells, by monitoring mitotic activity in timelapse videomicroscopy experiments. The compounds were screened for their antibacterial activity against gram-positive bacteria (Staphylococcus aureus var. Oxford 6538, Klebsielle pneumoniae ATCC 100131 and Legionella monocytogenes ATCC 35182), gram-negative bacteria (Escherichia coli ATCC 10536, Pseudomonas aeruginosa ATCC 9027 and Salmonella typhimurium ATCC 14028) and anti-fungal activity (Candida albicans and Aspergillus flavus) using paper disc diffusion technique. The minimum inhibitory concentrations (MICs) of the compounds were also determined by agar streak dilution method. Compounds 3 and 4 proved to be the most effective as antibacterial agents. The antiproliferative activity was investigated by counting the number of mitoses for HeLa, and MCF7 cells. No significant antiproliferative effect was noted for HL and complex 2, for both used cell types. For complexes 1 and 3 complete inhibition of cell proliferation was observed in the case of HeLa cells, while the effects on MCF7 cell proliferation were lower. In conclusion, six new complex compounds were synthesized, and their biological activity investigated on both prokaryotic and eukaryotic cells, proving that some of them could be putative therapeutic substances.
authors.affiliation: Inorganic Chemistry Department, Faculty of Chemistry, University of Bucharest, 23 Dumbrava Rosie Street, 050107 Bucharest, Romania. rosutudor51@yahoo.com
authors.forename: Tudor
authors.initials: T
authors.lastname: Rosu
authors.forename: Elena
authors.initials: E
authors.lastname: Pahontu
authors.forename: Diana-Carolina
authors.initials: DC
authors.lastname: Ilies
authors.forename: Rodica
authors.initials: R
authors.lastname: Georgescu
authors.forename: Mihaela
authors.initials: M
authors.lastname: Mocanu
authors.forename: Mircea
authors.initials: M
authors.lastname: Leabu
authors.forename: Sergiu
authors.initials: S
authors.lastname: Shova
authors.forename: Aurelian
authors.initials: A
authors.lastname: Gulea
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects*; D049109:Cell Proliferation / Q000187:drug effects; D060326:Chemistry Techniques, Synthetic; D003300:Copper / Q000737:chemistry; D005658:Fungi / Q000187:drug effects*; D006367:HeLa Cells; D006801:Humans; D007211:Indoles / Q000737:chemistry*; D019216:Metals, Heavy / Q000737:chemistry*; D009532:Nickel / Q000737:chemistry; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D012545:Schiff Bases / Q000737:chemistry; D014639:Vanadium / Q000737:chemistry
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D000970:Antineoplastic Agents; D007211:Indoles; D019216:Metals, Heavy; D009942:Organometallic Compounds; D012545:Schiff Bases; D014639:Vanadium; D003300:Copper; C012381:indole-3-carbaldehyde; D009532:Nickel