Facultatea de Chimie şi Tehnologie Chimică / Faculty of Chemistry and Chemical Technology

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Author: search.filters.author.Pahonțu, ElenaSubject: search.filters.subject.antiproliferative activity

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    NOVEL 2-FORMYLPYRIDINE 4-ALLYL-S- METHYLISOTHIOSEMICARBAZONE AND ZN(II), CU(II), NI(II) AND CO(III) COMPLEXES: SYNTHESIS, CHARACTERIZATION, CRYSTAL STRUCTURE, ANTIOXIDANT, ANTIMICROBIAL AND ANTIPROLIFERATIVE ACTIVITY
    (2019) Balan, Greta; Usataia, Irina; Graur, Vasilii; Ciumacov, Iurie; Petrenko, Peter; Gudumac, Valentin; Gulea, Aurelian; Pahonțu, Elena; Burduniuc, Olga
    New zinc (II), copper (II), nickel (II) and cobalt (III) complexes, [Zn (HL)2]I2 (1), [Cu (HL)Cl2] (2), [Cu (HL)Br2] (3), [Cu (HL)(H2O)2](ClO4)2 (4), [Ni (HL)2]I2·H2O (5), [Co(L)2]Cl (6), [Co(L)2]NO3 (7), [Co(L)2]I·[Co(L)2](I3) (8) were obtained with 2-formylpyridine 4-allyl-S-methylisothiosemicarbazone (HL). The isothiosemicarbazone ligand was characterized by NMR (1H and 13C), IR spectroscopy and X-ray diffraction. All the complexes were characterized by elemental analysis, IR, UV–Vis, ESI-MS spectroscopy, molar conductivity, magnetic susceptibility measurements. X-ray diffraction analysis on the monocrystal and powder elucidated the structure of the complexes 1, 5, 7 and 8. The ligand and the complexes were tested for their antioxidant and antimicrobial activity against Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae and Candida albicans. Also, the antiproliferative properties of these compounds on human leukemia HL-60, human cervical epithelial HeLa, human epithelial pancreatic adenocarcinoma BxPC-3, human muscle rhabdomyosarcoma spindle, large multinucleated RD cells and normal MDCK cells have been investigated. The nickel complex 5 and cobalt complexes 6, 7 showed promising antiproliferative activity and low toxicity.
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    SYNTHESIS, CHARACTERIZATION, CRYSTAL STRUCTURE OF NOVEL CU (II), CO (III), FE (III) AND CR (III) COMPLEXES WITH 2‐ HYDROXYBENZALDEHYDE‐4‐ALLYL‐S‐METHYLISOTHIOSEMICARBAZONE: ANTIMICROBIAL, ANTIOXIDANT AND IN VITRO ANTIPROLIFERATIVE ACTIVITY
    (2018) Pahonțu, Elena; Usataia, Irina; Graur, Vasilii; Ciumacov, Iurie; Petrenko, Peter; Gudumac, Valentin; Gulea, Aurelian
    2-Hydroxybenzaldehyde-4-allyl-S-methylisothiosemicarbazone and Cu (II), Co (III), Fe (III) and Cr (III) complexes were synthesized and characterized. The new obtained compounds were investigated by elemental analysis, magnetic susceptibility measurements, molar electric conductivity, IR, 1H NMR, 13C NMR, UV–Vis spectroscopy. In addition, the structure of the ligand and six complexes has been determined by single-crystal X-ray diffraction analysis. The Cu atom in complex 3 is penta-coordinated in a distorted square–pyramidal coordination geometry, while the metals in complexes 5–9 are in a distorted octahedral environment. For all compounds the antimicrobial activity was studied on a series of standard strains, such as Staphylococcus aureus, Escherichia coli, Enterococcus faecalis, Salmonella abony and Candida albicans. The in vitro antiproliferative activity of the ligand and complexes was screened on human leukemia HL-60 cells, human cervical epithelial HeLa cells, human epithelial pancreatic adenocarcinoma BxPC-3 cells, human muscle rhabdomyosarcoma spindle and large multinucleated RD cells. The primary screening on a wider series of cancer cells showed that copper coordination compound 2 manifests high activity towards HeLa, BxPC-3 and RD cancer cells, which is three–six times higher than the activity of doxorubicin. The selectivity index that is the ratio between the IC50 value for the normal MDCK cells and IC50 values for the cancer cells varies in the range 2.44–21.17. This index is 5.5–11 times higher for the copper coordination compound 2 than for the doxorubicin. Cr (III), Fe (III) and Co (III) coordination compounds 6–9 manifest high antioxidant activity towards ABTS•+ that exceeds 47–67 times the activity of Trolox.
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    ANTIBACTERIAL, ANTIFUNGAL AND IN VITRO ANTILEUKAEMIA ACTIVITY OF METAL COMPLEXES WITH THIOSEMICARBAZONES
    (Wiley, 2015) Pahonțu, Elena; Julea, Felicia; Rosu, Tudor; Purcarea, Victor; Chumakov, Yurie; Petrenco, Petru; Gulea, Aurelian
    1-phenyl-3-methyl-4-benzoyl-5-pyrazolone 4-ethyl-thiosemicarbazone (HL) and its copper(II), vanadium(V) and nickel(II) complexes: [Cu(L)(Cl)]·C2H5OH·(1), [Cu(L)2]·H2O (2), [Cu(L)(Br)]·H2O·CH3OH (3), [Cu(L)(NO3)]·2C2H5OH (4), [VO2(L)]·2H2O (5), [Ni(L)2]·H2O (6), were synthesized and characterized. The ligand has been characterized by elemental analyses, IR, 1H NMR and 13C NMR spectroscopy. The tridentate nature of the ligand is evident from the IR spectra. The copper(II), vanadium(V) and nickel(II) complexes have been characterized by different physico-chemical techniques such as molar conductivity, magnetic susceptibility measurements and electronic, infrared and electron paramagnetic resonance spectral studies. The structures of the ligand and its copper(II) (2, 4), and vanadium(V) (5) complexes have been determined by single-crystal X-ray diffraction. The composition of the coordination polyhedron of the central atom in 2, 4 and 5 is different. The tetrahedral coordination geometry of Cu was found in complex 2 while in complex 4, it is square planar, in complex 5 the coordination polyhedron of the central ion is distorted square pyramid. The in vitro antibacterial activity of the complexes against Escherichia coli, Salmonella abony, Staphylococcus aureus, Bacillus cereus and the antifungal activity against Candida albicans strains was higher for the metal complexes than for free ligand. The effect of the free ligand and its metal complexes on the proliferation of HL-60 cells was tested.