Contacts:
Supervisor(s):
Gabbiani Chiara, Pratesi Alessandro
Title of the PhD project:
Activatable Pt(IV) compounds as potential anticancer prodrugs
Abstract of the PhD project:
Cisplatin and its derivatives are anticancer drugs currently used in therapy whose mechanism of action mainly consists in the binding to the nucleic acids. However, despite their efficacy, they show several side effects. On the other hand, Pt(IV) complexes are kinetically more inert than the Pt(II) counterparts, and thus less toxic. These complexes act as prodrugs which can be activated inside the cancer cells through reduction, thus releasing the active Pt(II) drug and the two axial ligands. The Pt(II) species are responsible for the cytotoxicity but the introduction of bioactive axial ligands might further improve the pharmacological properties of these molecules. This project aims to the synthesis of new Pt(IV) complexes with bioactive axial ligands which, thorough reduction directly on the tumour site, could release the active molecules in situ, thus limiting the diffused side effects related to traditional Pt compounds. In this context, the new Pt(IV) complexes will be synthesized through the oxidation of Pt(II) precursors. Moreover, the possibility of administrating photoactivatable Pt(IV) complexes could be useful for on-site selective activation.
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