|
|||||
|
|
124I Radiolabeling of a AuIII-NHC Complex for In Vivo Biodistribution Studies |
|
| Authors: | Federica Guarra Alessio Terenzi Christine Pirker Rossana Passannante Dina Baier Ennio Zangrando Vanessa Gómez-Vallejo Tarita Biver Chiara Gabbiani Walter Berger Jordi Llop Luca Salassa |
| Affiliation: | 1. Department of Chemistry and Industrial Chemistry, University of Pisa, Via G. Moruzzi 13, 56124 Pisa, Italy These authors contributed equally to this work.;2. Donostia International Physics Center, Paseo M. Lardizabal 4, 20018 Donostia, Spain;3. Department of Medicine I, Institute of Cancer Research and Comprehensive Cancer Center, Medical University Vienna, Borschkegasse 8a, 1090 Vienna, Austria;4. CIC biomaGUNE, Basque Research and Technology Alliance (BRTA), Paseo de Miramón 182, 20014 Donostia, Spain;5. Department of Medicine I, Institute of Cancer Research and Comprehensive Cancer Center, Medical University Vienna, Borschkegasse 8a, 1090 Vienna, Austria Institute of Inorganic Chemistry, Faculty of Chemistry University of Vienna, Waehringerstrasse 42, 1090 Vienna, Austria;6. Department of Chemical and Pharmaceutical Sciences, University of Trieste, via Giorgieri 1, 34127 Trieste, Italy;7. Department of Chemistry and Industrial Chemistry, University of Pisa, Via G. Moruzzi 13, 56124 Pisa, Italy Department of Pharmacy, University of Pisa, via Bonanno 6, 56126 Pisa, Italy;8. Department of Chemistry and Industrial Chemistry, University of Pisa, Via G. Moruzzi 13, 56124 Pisa, Italy |
| Abstract: | AuIII complexes with N-heterocyclic carbene (NHC) ligands have shown remarkable potential as anticancer agents, yet their fate in vivo has not been thoroughly examined and understood. Reported herein is the synthesis of new AuIII-NHC complexes by direct oxidation with radioactive [124I]I2 as a valuable strategy to monitor the in vivo biodistribution of this class of compounds using positron emission tomography (PET). While in vitro analyses provide direct evidence for the importance of AuIII-to-AuI reduction to achieve full anticancer activity, in vivo studies reveal that a fraction of the AuIII-NHC prodrug is not immediately reduced after administration but able to reach the major organs before metabolic activation. |
| Keywords: | anticancer metallodrugs N-heterocyclic carbenes positron emission tomography radiochemistry |