2. Articole

Permanent URI for this collectionhttps://msuir.usm.md/handle/123456789/46

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Author: search.filters.author.Gulea, AurelianSubject: search.filters.subject.cancer cells

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    SYNTHESIS, CHARACTERIZATION, AND BIOLOGICAL ACTIVITY OF NOVEL 3d METAL COORDINATION COMPOUNDS WITH 2-ACETYLPYRIDINE N4-allyl-S-METHYLISOTHIOSEMICARBAZONE
    (Wiley, 2021) Graur, Vasilii; Usataia, Irina; Bourosh, Pavlina; Kravtsov, Victor; Garbuz, Olga; Hureau, Christelle; Gulea, Aurelian
    New zinc(II), copper(II), nickel(II), iron(III), and cobalt(III) coordination compounds, [Zn(HL)I2] (1), [Cu(HL)Cl2] (2), [Cu(HL)Br2] (3), {[Cu(HL)NO3]NO3}n (4), [Ni(HL)2](NO3)2 (5), [Fe(L)2]NO3(6), [Co(L)2]NO3 (7), and [Co(L)2]Cl·H2O (8), were obtained with 2-acetylpyridine N4-allyl-S-methylisothiosemicarbazone (HL). The isothiosemicarbazone proligand was characterized by nuclear magnetic resonance (NMR) (1H and 13C), infrared (IR) spectroscopy, and X-ray diffraction. All the coordination compounds were characterized by elemental analysis, IR, UV–Vis spectroscopy, molar conductivity, and magnetic susceptibility measurements. Single-crystal X-ray diffraction analysis elucidated the structure of the cationic form of the proligand in the salt [H2L]I and compounds 1–4 and 8 and demonstrated an unusual way of coordination through methylated sulfur atom in 1 and 3. Nevertheless, the electron paramagnetic resonance (EPR) and UV–Vis investigations showed that this way of coordination quickly changes upon dissolution of coordination compounds in dimethyl sulfoxide (DMSO). The antiproliferative properties of these compounds towards human cervical epithelial HeLa, human epithelial pancreatic adenocarcinoma BxPC-3, human muscle rhabdomyosarcoma spindle, large multinucleated RD cancer cell lines, and normal kidney epithelial MDCK cell line have been investigated. Copper coordination compounds (2–4) show promising anticancer activity with high selectivity (selectivity index [SI] = 10–18) towards BxPC-3 cell line. They also possess significant antibacterial and antifungal activity, which is useful for cancer treatment.
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    SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL ACTIVITY OF COPPER(II), NICKEL(II), COBALT(III) AND IRON(III) COORDINATION COMPOUNDS WITH 2-HYDROXY-3-METHOXYBENZALDEHYDE N(4)-ALLYL-S-METHYLISOTHIOSEMICARBAZONE
    (CEP USM, 2018) Usataia, Irina; Graur, Vasilii; Tsapcov, Victor; Gulea, Aurelian
    The paper presents the synthesis of the 2-hydroxy-3-methoxybenzaldehyde N(4)-allyl-S-methylisothiosemicarbazone (HL) and seven coordination compounds of copper, nickel, cobalt and iron with this ligand. The new obtained compounds were studied using IR, 1H and 13C NMR spectroscopy, elemental analysis, molar electric conductibility and magnetic susceptibility. The in vitro antiproliferative activity of the HL and synthesized coordination compounds was screened on HeLa cancer cells and normal MDCK cells. The isothiosemicarbazone HL shows better anticancer activity towards HeLa cancer cells than doxorubicin that is used in medical practice and it also practically does not affect the growth and proliferation of normal cells. Moreover, it manifests high antioxidant activity towards ABTS•+ radical cation that exceeds the activity of trolox.
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    STRUCTURE OF 2 - [ - 3 - (4 - METHYLPHENYL) - 1 - (PYRI DIN - 2 - YL)PROP - 2 - EN - 1 - YLIDENE]HYDRAZINE - 1 - CARBOTHIOAMIDE
    (2018) Rusnac, R.; Petrenco, P.; Chumakov, Yu.; Botnaru, Maria; Gulea, Aurelian
    During the recent years, a large number of chalcone-derived thiosemicarbazones are found to have potential therapeutic applications. They possess diverse biological activities including anti-inflammatory, antimicrobial and as cell growth inhibitor. It was found that the biological properties of these complexes correlate with their structures and the metal coordination leads to an improvement of chalcone-thiosemicarbazones pharmacological activities and synergistic effects. The aim of this work is the synthesis and the determination of structural and biological properties of 2-[-3-(4-methylphenyl)-1-(pyridin-2-yl)prop-2-en-1-ylidene]hydrazine-1-carbothioamide (I). In C=N-NH-CS backbone of I the S atom is in trans to azomethine N atom. This core of the studied ligand is essentially planar within 0.01 Ǻ. In I the dihedral angles of aromatic rings with mentioned backbone are equal to 30.0 and 32.2° respectively. In the crystal the molecules form the centro symmetric dimers via N-HS hydrogen bonds which in turn join through the N-H…N H-bonds. The synthesized compound I shows the moderate inhibition of HeLa, BxPC-3, TC-1 cancer cells in the range of concertation of 10-1 μM.
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    SINTEZA ŞI CERCETAREA PROPRIETĂŢILOR BIOLOGICE ALE UNOR DERIVAŢI AI 4-AMINO-5-METIL-4H-1,2,4-TRIAZOLULUI-3-TIOL
    (CEP USM, 2016) Rusnac, Anna; Rusnac, Roman; Garbuz, Olga; Babără, Nicanor; Gulea, Aurelian
    În prezenta lucrare a fost realizată sinteza1,1-dimetil-3-(3-metil-5-sulfanil-4H-1,2,4-triazol-4-il)tioureei (5) şi a1,1-dimetil-3-[3-metil-5-(metilsulfanil)-4H-1,2,4-triazol-4-il]tioureei (6), ale căror structuri au fost stabilite cu ajutorul spectrelor 1H-RMN şi 13C-RMN. Pe celule de cancer cervical substanţele iodhidrat de 3-metil-5-(metilsulfanil)-4H-1,2,4-triazol-4-amină 2) şi 6 au demonstrat o activitate nesemnificativă. Disulfura de tetrametiltiuram(DTMT) a demonstrat rezultate antibacteriene bune CMI 0,0007 mg/mL,iar substanţele 6 şi 2 au CMI 0,007 mg/mL şi, respectiv, 0,06 mg/mL. Tioureea 6 are proprietăţi antioxidante IC50= 29 μM/L aproximativ egale cu ale troloxului.A fost realizată sinteza N-[4-(3-metil-7H-1,2,4]triazolo[3,4-b][1,3,4]-tiadiazin-6-il)fenil]-2-[1-(piridin--il)etiliden]hidrazincarbotioamidei (11) şi a bazei Schiff [{[3-metil-5-(metilsulfanil)-4H-1,2,4-triazol-4-il]imino}metil]fenol (3). La compusul 3a fost efectuată difracţia cu raze X în monocristal.