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

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Author: search.filters.author.Garbuz, OlgaSubject: search.filters.subject.antiproliferative activity

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    NOVEL COPPER(II) COMPLEXES WITH N4,S-DIALLYLISOTHIOSEMICARBAZONES AS POTENTIAL ANTIBACTERIAL/ANTICANCER DRUGS
    (2023) Graur, Vasilii; Usataia, Irina; Graur, Ianina; Garbuz, Olga; Bouroș, Paulina; Cravțov, Victor; Lozan-Tîrșu, Carolina; Balan, Greta; Fala, Valeriu; Gulea, Aurelian
    The six new copper(II) coordination compounds [Cu(HL1)Cl2] (1), [Cu(HL1)Br2] (2), [Cu(H2O)(L1)(CH3COO)]·1.75H2O (3), [Cu(HL2)Cl2] (4), [Cu(HL2)Br2] (5), [Cu(H2O)(L2)(CH3COO)] (6) were synthesized with 2-formyl- and 2-acetylpyridine N4,S-diallylisothiosemicarbazones (HL1 and HL2). The new isothiosemicarbazones were characterized by NMR, FTIR spectroscopy, and X-ray crystallography ([H2L2]I). All copper(II) coordination compounds were characterized by elemental analysis, FTIR spectroscopy, and molar conductivity of their 1mM methanol solutions. Furthermore, the crystal structure of complex 3 was determined using single-crystal X-ray diffraction analysis. The studied complexes manifest antibacterial and antifungal activities, that in many cases are close to the activity of medical drugs used in this area, and in some cases even exceed them. The complexes 4 and 5 showed the highest indexes of selectivity (280 and 154) and high antiproliferative activity against BxPC-3 cell lines that surpass the activity of Doxorubicin. The complexes 1–3 also manifest antioxidant activities against cation radicals ABTS•+ that are close to that of trolox, the antioxidant agent used in medicine.
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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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    SINTEZA ȘI STUDIUL UNOR N'-(n-DIMETILFENIL)-N,N-DIMETILTIOUREI ȘI N(4)-n-DIMETILFENIL-TIOSEMICARBAZIDE
    (CEP USM, 2017) Erhan, Tatiana; Garbuz, Olga; Gulea, Aurelian
    În lucrare este descrisă sinteza și activitatea antiproliferativă a 6 tiourei și a 6 tiosemicarbazide. Puritatea și identitatea compușilor obținuți a fost confirmată cu ajutorul spectroscopiei1H și 13C RMN, IR, cromatografieipe strat subțire CSS și al temperaturii de topire.Toate substanțele sintetizate au fost testate in vitro, pentru activitatea antiproliferativă pe liniile celulare umane de cancer, și anume: carcinom cervical (HeLa), carcinom pancreatic (BxPc-3), rhabdomiosarcomă(RD) și celule sănătoase de MDCK. S-a urmărit studiul relației structură-activitate.