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RESEARCH PRODUCT
124I Radiolabeling of a AuIII‐NHC Complex for In Vivo Biodistribution Studies†
Jordi LlopTarita BiverRossana PassannanteWalter BergerChristine PirkerDina BaierFederica GuarraAlessio TerenziAlessio TerenziVanessa Gómez-vallejoEnnio ZangrandoLuca SalassaLuca SalassaLuca SalassaChiara Gabbianisubject
Imaging Agents | Hot Paperpositron emission tomography010405 organic chemistryChemistryGeneral ChemistryProdrug010402 general chemistryanticancer01 natural sciencesCombinatorial chemistryCatalysisIn vitro3. Good health0104 chemical sciencesIn vivoIn vivo biodistributionSettore CHIM/03 - Chimica Generale E InorganicametallodrugsN-heterocyclic carbenesanticancer; metallodrugs; N-heterocyclic carbenes; positron emission tomography; radiochemistryradiochemistryResearch ArticlesResearch Articledescription
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.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2020-01-01 | Angewandte Chemie (International Ed. in English) |