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Biometals ; 28(5): 845-60, 2015 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-26091950

RESUMO

Novel gold(I) and gold(III) complexes containing derivatives of D-galactose, D-ribose and D-glucono-1,5-lactone as ligands were synthesized and characterized by IR, (1)H, and (13)C NMR, high resolution mass spectra and cyclic voltammetry. The compounds were evaluated in vitro for their cytotoxicity against three types of tumor cells: cervical carcinoma (HeLa) breast adenocarcinoma (MCF-7) and glioblastoma (MO59J) and one non-tumor cell line: human lung fibroblasts (GM07492A). Their antitubercular activity was evaluated as well expressed as the minimum inhibitory concentration (MIC90) in µg/mL. In general, the gold(I) complexes were more active than gold(III) complexes, for example, the gold(I) complex (1) was about 8.8 times and 7.6 times more cytotoxic than gold(III) complex (8) in MO59J and MCF-7 cells, respectively. Ribose and alkyl phosphine derivative complexes were more active than galactose and aryl phosphine complexes. The presence of a thiazolidine ring did not improve the cytotoxicity. The study of the cytotoxic activity revealed effective antitumor activities for the gold(I) complexes, being more active than cisplatin in all the tested tumor cell lines. Gold(I) compounds (1), (2), (3), (4) and (6) exhibited relevant antitubercular activity even when compared with first line drugs such as rifampicin.


Assuntos
Carboidratos/química , Proliferação de Células/efeitos dos fármacos , Complexos de Coordenação/química , Ouro/química , Carboidratos/administração & dosagem , Carboidratos/síntese química , Cisplatino/administração & dosagem , Complexos de Coordenação/síntese química , Complexos de Coordenação/farmacologia , Fibroblastos/efeitos dos fármacos , Fibroblastos/patologia , Ouro/administração & dosagem , Células HeLa , Humanos , Ligantes , Pulmão/efeitos dos fármacos , Pulmão/patologia , Células MCF-7 , Espectroscopia de Ressonância Magnética , Rifampina/administração & dosagem , Relação Estrutura-Atividade
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