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

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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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    SINTEZA COMBINAȚIILOR COORDINATIVE NOI ALE UNOR METALE 3D ÎN BAZA N(4)-(ACETAT DE ETIL) TIOSEMICARBAZONELOR 2-FORMIL ȘI 2-ACETIL PIRIDINEI. PROPRIETĂȚI ANTIOXIDANTE
    (2022) Rusnac, Anna; Garbuz, Olga; Șova, Sergiu; Gulea, Aurelian
    The given work includes the description of methods for the synthesis of new coordinative combinations of Cu(II), Mn(II), Fe(III) Co(III), Ni(II) and Zn(II) with N(4)-(ethyl acetate) thiosemicarbazones of 2-formylpyridine and 2-acetylpyridine. The characterization of the newly synthesized compounds was carried out using 1H NMR, 13C NMR, FTIR spectroscopy, conductivity, and elemental analysis. In addition, the structures of N(4)-(ethyl acetate) thiosemicarbazide and N(4)-(ethyl acetate) thiosemicarbazone 2-acetylpyridine (HL2) were determined using single crystal X-ray diffraction. The antioxidant activity of coordinative combinations was studied and compared with that of free ligands. The most pronounced antioxidant properties are possessed by [Ni(L2)Cl], whose value of IC50=15,05 μM is three times higher than the IC50=46,76 μM of the non-coordinating ligand and about 2,5 times higher than the reference substances Rutin and Trolox.
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    IN VITRO ANTIPROLIFERATIVE ACTIVITY AND ANTIOXIDANT CAPACITY OF NEW ORGANOMETALLIC COORDINATION COMPOUNDS, RESULTS CORRELATION ANALYSIS
    (2016) Gulea, Aurelian; Gudumac, Valentin; Garbuz, Olga; Andronache, Lilia
    A fost examinată și testată capacitatea inhibitorilor organometalici activi CMJ-33, CMSA-4, de a induce apoptoza în celulele epiteliale de carcinom de col uterin linia HeLa. Viabilitatea celulelor canceroase a fost determinată prin testul Alamar Blue fiind folosit un indicator redox – resazurin. S-a depistat activitate antitumorală mai mare a substanțelor testate decât la cea luată în calitate de etalon: - doxorubicina (DOXO). În scopul de a detecta eventuala prezenţă a efectelor adverse concomitente legate cu proprietățile pro-oxidante ale compușilor coordinativi, a fost folosită metoda cantitativă ORAC (Oxygen Radical Absorption Capacity). Rezultatele au demonstrat că substanțele testate CMT-67 şi CMSA-4 posedă activitate antioxidantă mai mare decât Trolox și DOXO. În această lucrare, noi constatăm prezența unei corelații pozitive semnificative (coeficient de corelație - 0,98) între efectele anti-proliferative și anti-oxidante pentru compuşii CMT-67, CMSA-4 și DOXO.
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    SYNTHESIS AND BIOLOGICAL ACTIVITY OF 2-FORMYLPYRIDINE N(4)-ALLYL-3-SELENO-SEMICARBAZONE AND ITS COPPER COORDINATION COMPOUND
    (2015) Graur, Vasilii; Garbuz, Olga; Zariciuc, Elena; Gudumac, Valentin; Gulea, Aurelian
    The paper presents the synthesis of the 2-formylpyridine N(4)-allyl-3-seleno-semicarbazone that was studied using NMR spectroscopy. This ligand was used for the synthesis of a copper(II) chloride coordination compound. The study of antimicrobial and antifungal activities showed that these substances possess bacteriostatic and bactericidal activities towards a series of gram-positive and gram-negative bacteria and fungi in the range of concentration 0.7-500μg/mL. The activity of the copper(II) coordination compound towards gram-negative microorganisms significantly exceeds the activity of the ligand. The antioxidant activity of the synthesized selenosemicarbazones exceeds the activity of the coordination compound. These substances inhibit proliferation of MeW-164, HL-60 and HeLa tumor cells. 16 references, 1 table, 7 schemes
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    EVALUAREA BIOLOGICĂ A COMPUȘI LOR COORDINATIVI AI CUPRULUI(II) CU UNELE TIOSEMICARBAZONE HETEROCICLICE
    (CEP USM, 2022) Garbuz, Olga; Railean, Nadejda; Gostev, Igor; Rusnac, Anna; Toderaş, Ion; Gulea, Aurelian
    Au fost sintetizați 3 compuși noi: tiosemicarbazona 2-acetilpiridinei H2L, cloro(tiosemicarbazona-2-acetilpiridinei) cupru(II) (1) și nitrato(tiosemicarbazona-2-acetilpiridinei)cupru(II) (2) care potențial posedă proprietăți antiproliferative fată de celulele canceroase. Doxorubicina (7-[4-amino-5-hidroxi-6-metiloxan-2-il]oxi-6,9,11-trihidroxi-9-(2-hidroxiacetil)4-metoxi-8,10-dihidro-7H-tetracen-5,12-dionă) a fost utilizată în calitate de compus anticancerigen de referință și Trolox (acid 6-hidroxi-2,5,7,8-tetramethilcroman-2-carboxilic) a fost utilizat ca compus antioxidant de referință. Compușii testați au demonstrat efect antioxidant înalt față de cationii radicali ABTS•+ în comparație cu interacțiunea acestor cationi cu Trolox. Compușii testați au manifestat toxicitate generală față de Daphnia magna după 24 de ore de expunere cu determinarea unui șir de descreștere. Datele experimentale au indicat perspectivele pentru viitoare căutări ale substanțelor anticancerigene selective cu acțiune antioxidantă înaltă și toxicitate scăzută.