Recent developments in the field of platinum anticancer drugs have revealed that compounds containing derivates of pyridine may exhibit highly cytotoxic activity against a variety of tumor cells, with AMD473 (cis-PtCl(2)(NH(3))(2-methylpyridine)) as one of the most relevant examples. Following these advances, this paper describes the synthesis, characterization and X-ray structure of the square-planar compound cis-[Pt(3-Acpy)(2)Cl(2)] (1, Acpy stands for acetylpyridine), where the coordination of 3-acetylpyridine takes places through the pyridine nitrogen of the ligand. The structural arrangement of this compound is highly peculiar and it is the first example with two of these 3-acetylpyridine molecules in a cis disposition. In addition, the anticancer and antibacterial activities of this compound together with studies of DNA binding are also described in detail, with selective activity of compound 1 against A2780R cells. cis-[Pt(3-Acpy)(2)Cl(2)] apparently coordinates to the DNA double helix upon exchange of at least one of the Cl(-) ions with the media and shows very interesting bacteriolytic and bacteriostatic activity against Escherichia coli and Streptomyces, respectively.