Abstract

Copper coordination complexes are increasingly recognized as potential drugs for therapeutic use in various diseases, especially in cancer. In an attempt to find new leaders for the development of antitumor Cu compounds, heteroleptic Cu(I) complexes with triphenylphosphine (PPh3) and dimethylbipyridine (dmbpy), phenanthroline (phen) or neocuproine (neo) were prepared and characterized. The compounds [CuCl(dmbpy)(PPh3)] (1), [CuCl(phen)(PPh3)]⋅0,25H2O (2) and [CuCl(neo)(PPh3)] (3) were obtained. The crystal structures of compounds 2 and 3 were determined. In both complexes, the Cu(I) centre presents distorted tetrahedral coordination. All complexes present cytotoxic activity, against tumor cell lines, being more active than Cisplatin, with IC50 in the low micromolar range. This activity augments in the order 1<2<3, following the same order as the lipophilicity.

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