Objectif The ultimate objective of this research work is the preparation and evaluation of novel gold(III)-di/tripeptidedithiocarbamato complexes for combating cancer through their enhanced selective delivery at the tumor target site supported by transporter proteins. Platinum(II) drugs are now established as effective antitumour agents, the archetypal example of these being cisplatin. However, their usefulness is limited by their narrow spectrum of activity (not active enough against several types of cancer), and by both the development of acquired resistance after continuous treatment and toxicity (in particular, nephrotoxicity). Thus, several third-generation metal-based drugs have been prepared and tested. In this contest, gold(III) compounds are emerging as a new class of metal complexes with outstanding cytotoxic properties, and are presently being evaluated as potential antitumor agents. In particular, some gold(III)-dithiocarbamato derivatives were proved to be much more cytotoxic in vitro than cisplatin, and showed encouraging results in terms of both high in vivo effectiveness and lack of nephrotoxicity. This research project is concerned with the synthesis and characterization of new gold(III)-dithiocarbamato derivatives of di/tripeptides as improved peptide-based delivery systems, to be evaluated as antitumor drugs. The rationale behind our proposal is to design gold(III) complexes of the type [AuX2(pdtc)] (X = Cl, Br; pdtc = di/tripeptidedithiocarbamate) which can be able to both maintain the antitumor properties and the lack of nephrotoxicity of the previously reported gold(III) analogues, together with an enhanced bioavailability through the di/tripeptide-mediated cellular internalization promoted by transporter proteins. Thus, the enormous potential impact of this new class of gold(III) chemotherapeutic agents relies in their possible site-specific delivery in localized cancers strongly improving their cellular uptake and minimizing unwanted side-effects. Champ scientifique natural scienceschemical sciencesinorganic chemistrytransition metalsnatural sciencesbiological sciencesbiochemistrybiomoleculesproteinsmedical and health sciencesclinical medicineoncology Mots‑clés Anticancer therapy Inorganic chemistry Organometallic chemistry Pharmaceutical chemistry Programme(s) FP7-PEOPLE - Specific programme "People" implementing the Seventh Framework Programme of the European Community for research, technological development and demonstration activities (2007 to 2013) Thème(s) PEOPLE-2007-2-2.ERG - Marie Curie Action: "European Reintegration Grants" Appel à propositions FP7-PEOPLE-2007-2-2-ERG Voir d’autres projets de cet appel Régime de financement MC-ERG - European Re-integration Grants (ERG) Coordinateur UNIVERSITA DEGLI STUDI DI PADOVA Contribution de l’UE € 45 000,00 Adresse VIA 8 FEBBRAIO 2 35122 Padova Italie Voir sur la carte Région Nord-Est Veneto Padova Type d’activité Higher or Secondary Education Establishments Contact administratif Dolores Fregona (Prof.) Liens Contacter l’organisation Opens in new window Site web Opens in new window Coût total Aucune donnée