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

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    COORDINATION COMPOUNDS OF COBALT, NICKEL, COPPER, AND ZINC WITH N1,N2 -BIS(PYRIDIN-2-YLMETHYLIDENE)BENZENE-1,2-DIAMINE AND ITS DERIVATIVES
    (2014) Pahonțu, Elena; Gulea, Aurelian; Poirier, Donald; Țapcov, Victor
    o-Phenylenediamine reacts with 2-formyl-, 2-acetyl-, or 2-benzoylpyridine in ethanol in the presence of cobalt, nickel, copper, or zinc chlorides to form monomeric complexes ML1-3Cl2·nH2O {M = Co, Ni, Cu, Zn; L1 = N 1,N 2-bis(pyridin-2-ymethylidene)benzene-1,2-diamine, L2 = N 1,N 2-bis(pyridin-2-ylethylidene) benzene-1,2-diamine, L3 = N 1,N 2-bis[phenyl(pyridin-2-yl)methylidene]benzene-1,2-diamine; n = 0-3}. The condensation products (L1-L3) act in the complexes as tetradentate N,N,N,N-ligands. Thermolysis of the complexes occurs in two stages: dehydration (70-95°C) and complete degradation (320-450°C). At concentrations of 10-5-10-7 M, the complexes inhibit in vitro growth and proliferation of HL-60 human promyelocytic leukemia cells.
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    COORDINATION COMPOUNDS OF COPPER AND NICKEL WITH N,N'-[4,4'-(PERFLUORO-1,4-PHENYLENE)BIS(OXY)BIS(4,1-PHENYLENE)]- BIS[2-(PYRIDIN-2-YLMETHYLIDENE)HYDRAZINECARBOTHIOAMIDE] AND ITS DERIVATIVES
    (2014) Pahonțu, Elena; Țapcov, Victor; Poirier, Donald; Gulea, Aurelian
    N,N′-[4,4′-(Perfluoro-1,4-phenylene)bis(oxy)bis(4,1-phenylene)] bis[2-(pyridin-2-ylmethylidene)-hydrazinecarbothioamide] as well as its methyl and phenyl derivatives react with copper and nickel chlorides in ethanol to form coordination compounds. In the products, the hydrazinecarbothioamides act as doubly deprotonated bridging ligands. The prepared complexes have been found to inhibit in vitro the growth and propagation of the myeloid human leukemia HL-60 cancer cells at the 10-5-10-7 mol/L concentration.
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    SYNTHESIS, STRUCTURE, AND BIOLOGICAL ACTIVITY OF MIXED-LIGAND AMINE-CONTAINING COPPER(II) COORDINATION COMPOUNDS WITH 2-(2-HYDROXYBENZYLIDENE)-N-(PROP-2-EN-1-YL)HYDRAZINE- CARBOTHIOAMIDE
    (2021) Gulea, Aurelian; Graur, Vasilii; Ulchina, Ianina; Bouroș, Pavlina; Smaglii, Vadim; Garbuz, Olga; Țapcov, Victor
    Сopper(II) nitrate reacts in ethanol with 2-(2-hydroxybenzylidene)-N-(prop-2-en-1-yl)hydrazinecarbothioamide H2L in an 1 : 1 molar ratio to form the coordination compound Cu(HL)NO3·H2O. The introduction of amines [imidazole (Im), 3,5-dibromopyridine (3,5-Br2Py), and 4-methylpyridine (4-Pic)] into the reaction mixture in a molar ratio 1 : 1 : 2 leads to the formation of CuA(HL)NO3·nH2O [A = Im, 3,5-Br2Py, 4-Pic; n = 0, 3] complexes. The structure of the obtained compounds was determined by X-ray structural analysis. The synthesized complexes exhibit antimicrobial, antifungal, antioxidant, and anticancer activities.
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    SYNTHESIS, STRUCTURE AND BIOLOGICAL ACTIVITY OF COORDINATION COMPOUNDS OF COPPER, NICKEL, COBALT, AND IRON WITH ETHYL N'-(2-HYDROXYBENZYLIDENE)-N-PROP-2-EN- 1-YLCARBAMOHYDRAZONOTHIOATE
    (2020) Gulea, Aurelian; Usataia, Irina; Graur, Vasilii; Ciumacov, Iurie; Petrenko, Peter; Balan, Greta; Burduniuc, Olga; Țapcov, Victor; Rudic, Valeriu
    N-(Prop-2-en-1-yl)hydrazonocarbothioamide reacts with iodoethane in methanol with further addition of 2-hydroxybenzaldehyde to form hydroiodide of carbamohydrazonothioate (HL·HI). The coordination compounds were obtained by interaction of HL or HL·HI with copper, nickel, cobalt and iron salts CuLХ·nH2O [X = Cl–, Br–, NO3–; n = 0–1], Ni(L)2·HI·CH3OH, Сo(L)2X [X = I–, NO3–] and Fe(L)2NO3. The structures of three complexes were established by single crystal X-ray analysis. The synthesized complexes exhibit selective antimicrobial and antifungal activity against a series of standard microorganisms and fungi in the concentration range of 30–500 μg/mL. In addition, nickel and iron complexes selectively inhibit the growth and proliferation of cancer cells and do not adversely affect normal cells.
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    NICKEL(II) COMPLEXES WITH PENTANE-2,4-DIONE BIS(4-ALLYLTHIOSEMICARBAZONE)
    (2020) Gulea, Aurelian; Graur, Vasilii; Ciumacov, Iurie; Petrenko, Peter; Garbuz, Olga; Țapcov, Victor; Gudumac, Valentin
    Reaction of pentane-2,4-dione with N-(prop-2-en-1-yl)hydrazinecarbothioamide at a 1: 2 molar ratio in ethanol resulted in the formation of a pyrazole derivative. The latter reacted with nickel perchlorate at a 1: 1 molar ratio to form the nickel complex with pentane-2,4-dione bis(4-allylthiosemicarbazone). The same type of nickel complex was obtained as a result of N-(prop-2-en-1-yl)hydrazinecarbothioamide reaction with pentane-2,4-dione and nickel nitrate at a 2: 1: 1 molar ratio. Antimicrobial, antifungal, antioxidant, and anticancer activities of the obtained compounds were studied.
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    SYNTHESIS, STRUCTURE, AND BIOLOGICAL ACTIVITY OF COPPER AND COBALT COORDINATION COMPOUNDS WITH SUBSTITUTED 2-(2-HYDROXYBENZYLIDENE)-N-(PROP-2-EN-1-YL)HYDRAZINE- CARBOTHIOAMIDES
    (2019) Gulea, Aurelian; Graur, Vasilii; Ciumacov, Iurie; Petrenko, Peter A.; Balan, Greta; Burduniuc, Olga; Țapcov, Victor; Rudic, Valeriu
    The reaction of N-(prop-2-en-1-yl)hydrazinecarbothioamide with substituted 2-hydroxybenzaldehydes afforded the corresponding Schiff bases which were used as ligands to obtain copper and cobalt coordination compounds Cu(NL1–6)X · n H2O (X = Cl−, NO3−; n = 0–3), Co(HL2)2NO3, and Co(NL6)2Cl. The structure of the isolated complexes was determined by NMR spectroscopy and X-ray analysis. The complexes were tested for antimicrobial and antifungal activity against S. aureus, E. coli, and yeast-like fungi. Inhibitory effect of the initial thioamides and their complexes against human myeloid leukemia HL-60 cancer cell line was also studied.
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    SINTEZA ȘI CERCETAREA PROPRIETĂȚILOR FARMACOFORE ALE UNOR N-(DIMETILFENIL) HIDRAZINCARBOTIOAMIDE
    (2023) Erhan, Tatiana; Garbuz, Olga; Ungur, Nicon; Gulea, Aurelian
    The present study was focused on the synthesis of some N-(dimethylphenyl)hydrazine carbothioamides 1-4, that contain the following N-substituents: 2,4-dimethylphenyl; 2,5-dimethylphenyl; 2,6-dimethylphenyl; 3,4-dimethylphenyl, to increase lipophilicity and N-(dimethylphenyl)-2-(pyridin-2-ylmethylidene)hydrazinecarbothioamides 5-8, analogous of Triapine. The structural formula of the compounds was characterized by means of spectroscopy: FT-IR, 1H-, and 13CRMN, and the molecular structure, for the first time, by means of X-ray diffraction. The study of antioxidant activity has shown that all compounds 1-8 are powerful antioxidants. N-(dimethylphenyl)-2-(pyridin2-ylmethylidene)hydrazinecarbothioamides 5-8 were tested as inhibitors of MCF-7 (breast cancer) cell proliferation. It was found that all the compounds exhibit activity comparable to that of Doxorubicin, among them the compound N-(2,5-dimethylphenyl)-2-(pyridin-2-ylmethylidene)hydrazinecarbothioamide 6, with IC50=0.8 μM/L, demonstrated the highest activity.
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    SYNTHESIS, STRUCTURE, AND BIOLOGICAL ACTIVITY OF MIXED-LIGAND AMINE-CONTAINING COPPER(II) COORDINATION COMPOUNDS WITH 2-(2-HYDROXYBENZYLIDENE)-N-(PROP-2-EN-1-YL)HYDRAZINECARBOTHIOAMIDE
    (2021) Gulea, А. P.; Graur, V. О.; Ulchina, Ia. I.; Bourosh, P. N.; Smagliic, V. A.; Garbuz, O. S.; Tsapkov, V. I.
    Сopper(II) nitrate reacts in ethanol with 2-(2-hydroxybenzylidene)-N-(prop-2-en-1-yl)hydrazinecarbo- thioamide H2L in an 1 : 1 molar ratio to form the coordination compound Cu(HL)NO3·H 2O. The introduction of amines [imidazole (Im), 3,5-dibromopyridine (3,5-Br2Py), and 4-methylpyridine (4-Pic)] into the reaction mixture in a molar ratio 1 : 1 : 2 leads to the formation of CuA(HL)NO3·nH 2O [A = Im, 3,5-Br 2Py, 4-Pic; n = 0, 3] com- plexes. The structure of the obtained compounds was determined by X-ray structural analysis. The synthesized complexes exhibit antimicrobial, antifungal, antioxidant, and anticancer activities.
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    ПРОТИВОРАКОВАЯ И ТОКСИЧЕСКАЯ АКТИВНОСТЬ НОВОГО СИНТЕЗИРОВАННОГО ВЕЩЕСТВА
    (Marina Sokolova Publishings, 2017) Гуля, А.П.; Тодераш, А.К.; Гудумак, В. С.; Цапков, В.И.; Гарбуз, О. С; Рошков, Е. В.; Сардарь, В. В; Тагадюк, О. К.
    В данной работе представлен ряд сравнительных биологических исследований нового синтезированного вещества CMT-122.Антипролиферативная активность этого вещества тестировалась надвух клеточных линиях. Установлено, что CMT-122 проявляет цитотоксичность в отношении RD(рабдомиосаркома) с IC50 - 1,1±0.1 μ mol / L и HeLa (аденокарцинома шейки матки) с IC50-8,3±2,0 μ mol/L. Сравнительное изучение CMT-122 и доксорубицина в отношении раковых клеточных линий показало, что CMT-122 сильнее ингибирует пролиферацию раковых клеток, чем DOX.Дополнительный эксперимент, направленный на оценку цитотоксического эффекта с использованием нормальной клеточной линии MDCK (Madin Darby Canine Kidney), показал, что CMT-122 практически не ингибирует пролиферацию и не вызывает гибель этой линии клеток.Токсичность вещества определяли спектрофотометрическим биоанализом на тест-объектах Parameciumcaudatum. Установлено, что LC50 для CMT-122 в 5 раз меньше, чем у DOX.
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    IN VITRO ANTICANCER ACTIVITY OF CHLORO(N-PHENYL-N'-[(PYRIDIN-2- YL)METHYLIDENE]CARBAMOHYDRAZONOTHIOATO) (4-AMINOBENZENE-1-SULFONAMIDE)COPPER
    (CEP USM, 2018) Garbuz, Olga
    This study was aimed to evaluate the antiproliferative activity of the mixed-ligand complex (chloro(N-phenyl-N'- [(pyridin-2-yl)methylidene]carbamohydrazonothioato)(4-aminobenzene-1-sulfonamide)copper) on several cancer cells of lines. It was established, that the copper(II) mixed-ligand complex exhibits the highest anticancer activity against MeW-164, HeLa, BxPC-3 and RD cells of lines with IC50 values of 1.0±0.2, 0.4±0.04, 1.7±0.2, 1.3±0.3 µM, respectively. A comparative study between the tested compound and DOXO in regard to cancer lines has established that the tested copper(II) mixed-ligand complex exhibits stronger inhibitory activity on cancer cells proliferation than doxorubicin and cisplatin.