2. Articole

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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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    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.