Synthesis, structural characterization and in vitro cytotoxicity of gold complexes with 2-(2-pyridyl)benzimidazole. Gold)III) vs. cold(I), mono- vs. binuclear derivatives

Gold compounds are attracting much interest because of their promising pharmacological activity against a series of diseases. Some of these complexes are reported to posses a great potential for cancer treatment, 1 showing important anti proliferative activity both in vitro and in vivo, probably involving thioredoxin reductase inhibition. 2 In this framework, a variety of gold(III) and gold(I) derivatives of 2-(2-pyridyl)benzimidazole (pbiH), both mono- and binuclear, have been synthesized, fully characterized and their biological properties investigated. All complexes show from good to excellent cytotoxic activity in vitro toward the human carcinoma cell line A2780, both sensitive, A2780/S, and resistant, A2780/R, to cisplatin, with IC50 values falling in the low micromolar, and in some case nanomolar, range. In general, the binuclear derivatives were found more active than the corresponding mononuclear ones. Particularly beneficial was joining into the same compound a gold(III) and a gold(I) centre. Reactivity with model proteins (Cytochrome C and Lysozyme) was also studied by ESI MS and UV-visible spectrometry. Methods and results of this study will be presented. Literature [1] Nbili S., Mini E., Landini I., Gabbiani C., Casini A., Messori L., med. Res. Rev., 2010, 30, 550-580. [2] Pratesi A., Gabbiani C., Ginanneschi M., Messori L., Chem. Common., 2010, 46, 7001-7003