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We report the cytotoxic effects obtained in HeLa cells of three newly synthesized platinum complexes containing both an O,O′-chelated acetylacetonate ligand and a sulfur ligand in the platinum coordination sphere, which show, by ¹H NMR, negligible reactivity with purine bases. These compounds induce cell death with [Pt(O,O′-acac)(γ-acac)(DMS)] being the most effective (IC₅₀=0.98±0.056 and 1.82±0.023μM for [Pt(O,O′-acac)(γ-acac)(DMS)] and cisplatin, respectively). About 50% of cells died after 5h treatment with 100μM [Pt(O,O′-acac)(γ-acac)(DMS)] whilst a 16h incubation was required to get the same results using 100μM cisplatin. Cellular accumulation measurements, after treatment with equimolar drug concentrations, indicated the major lipophilicity and cellular uptake of the new compounds. While the cytotoxicity of cisplatin was due to both intracellular accumulation and DNA binding, that of [Pt(O,O …