124I Radiolabeling of a AuIII-NHC Complex for In Vivo Biodistribution Studies

Alessio Terenzi, Alessio Terenzi, Vanessa Gómez-Vallejo, Walter Berger, Federica Guarra, Dina Baier, Rossana Passannante, Tarita Biver, Luca Salassa, Jordi Llop, Christine Pirker, Ennio Zangrando, Chiara Gabbiani

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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.
Lingua originaleEnglish
pagine (da-a)17130-17136
Numero di pagine7
RivistaANGEWANDTE CHEMIE. INTERNATIONAL EDITION
Volume59
Stato di pubblicazionePublished - 2020

All Science Journal Classification (ASJC) codes

  • Catalysis
  • Chemistry(all)

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    Terenzi, A., Terenzi, A., Gómez-Vallejo, V., Berger, W., Guarra, F., Baier, D., Passannante, R., Biver, T., Salassa, L., Llop, J., Pirker, C., Zangrando, E., & Gabbiani, C. (2020). 124I Radiolabeling of a AuIII-NHC Complex for In Vivo Biodistribution Studies. ANGEWANDTE CHEMIE. INTERNATIONAL EDITION, 59, 17130-17136.