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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.

Este trabalho descreve a síntese e a caracterização de onze novos complexos de platina(II), contendo como ligantes derivados da 1,2-fenilenodiamina, da N-benzil etilenodiamina, e da 2-ou 4-picolina. Os complexos foram preparados em rendimentos satisfatórios pela reação dos ligantes com K 2 [PtCl 4 ]. É descrita também a atividade citotóxica de um dos complexos de platina(II), em sete linhagens de células tumorais de origem humana, que se mostrou muito menos ativo do que a cisplatina.This work describes the synthesis and characterization of eleven new platinum(II) complexes having ligands derived from 1,2-phenylenediamine, N-benzyl ethylenediamine and 2-or 4-picoline. The complexes were prepared in satisfactory yields by reaction of K 2 [PtCl 4 ] with the appropriate ligand. The cytotoxic pre-screening of one of these complexes in seven human cancer cell lines showed that this compound is much less active than cisplatin.

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This work describes the synthesis and characterization of five new amine ligands and also the preparation and characterization of their respective platinum(II) complexes by reaction with K 2 PtCl 4 in water. These ligands were obtained by treatment of different halides or epoxides with ethylenediamine. Cytotoxic activity and cellular accumulation of three complexes were investigated in a human small-cell lung carcinoma cell line and its cisplatin resistant subline. The introduction of a spacer (cycle) between the two platinum atoms leads to a significant decrease in cytotoxic activity. At equitoxic doses, the intracellular platinum concentrations found