Recently, we have prepared a series of stable cationic gold (III) complexes1 (Scheme 1) with the 'pincer' iminophosphorane ligand (2-C6H4-PPh2=NPh) which resulted cytotoxic in vitro against HeLa-GFP human cervical carcinoma and immortalized leukemia Jurkat-GFP cells. They did not interact with DNA although 2 manifested a high reactivity toward mitochondrial proteins indicating a mode of action different to that of platinum(II) complexes. We will report on more detailed studies of derivatives 1 and 2 that have confirmed two different mechanims for cell death: apoptosis and necrosis. Surprinsingly, experiments with antioxidants and Jurkat cells without mitochondrial DNA have indicated that free radicals involved in the toxicity of 1 and 2 are not originated in the mitochondrial electron transport chain.We will also report on the synthesis and cytotoxic properties of new hydrophilic gold(III) complexes by modification of the iminophosphorane ligand (Scheme 2).                                    1. Contel et al. Inorg. Chem, 2009, 48, 1577.

Synthesis of hydrophilic iminophosphorane organogold (III) complexes:
Study of their cytotoxicity against solid tumors in vitro and their interaction with biomolecular targets

239th National Meeting (2010)

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Synthesis of hydrophilic iminophosphorane organogold (III) complexes: Study of their cytotoxicity against solid tumors in vitro and their interaction with biomolecular targets