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Spreckelmeyer, Sarah, Thomas, Sophie R. 
ORCID: https://orcid.org/0000-0003-1110-430X, Schuderer, Franziska, Pinto, Catarina I. G., Querino, Ana Luiza de Andrade, Böhm, Felix A., Park, Mihyun, Geppert, Christopher, Gorges, Christian, Mendes, Filipa and Casini, Angela
(2025)
N-Heterocyclic Carbenes as Ligands to 198Au(I)-Radiolabeled Compounds: A New Platform for Radiopharmaceutical Design.
Journal of Medicinal Chemistry, 68 (16).
pp. 17516-17526.
ISSN 0022-2623
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Abstract
The radionuclide 198Au, with a half-life of 2.7 days, emits γ radiation ideal for diagnostic purposes and generates β –particles suitable for effective cancer radiotherapy, making it a perfect nuclide for “theranostics”. However, the application of coordination compounds of Au(I)/Au(III) in medicine is limited by their instability in vivo. Here, we explore N-heterocyclic carbene (NHC) organometallic chemistry to stabilize 198Au(I) in radiopharmaceuticals. Thus, Au(I) NHC compounds featuring different scaffolds were selected for 198Au radiolabeling. Eventually, two compounds featuring imidazole (AuNHC-1) and theophylline (AuTMX 2) scaffolds were successfully radiolabeled (radiochemical purity = 92.9% and 40.2%, respectively). Instead, two peptidic Au(I) benzimidazolylidene derivatives, capable of blood–brain barrier translocation in vitro, were subjected to ligand exchange reactions under the applied radiolabeling conditions. The obtained proof-of-concept results showed that NHCs are suitable ligands to achieve isotope exchange in Au(I) complexes. Overall, our work reveals the still untapped potential of organometallic chemistry in radiopharmaceutical design.
| Item Type: | Article |
|---|---|
| Faculty \ School: | Faculty of Science > School of Chemistry, Pharmacy and Pharmacology |
| Related URLs: | |
| Depositing User: | LivePure Connector |
| Date Deposited: | 14 Sep 2026 15:53 |
| Last Modified: | 14 Sep 2026 20:09 |
| URI: | https://ueaeprints.uea.ac.uk/id/eprint/104523 |
| DOI: | 10.1021/acs.jmedchem.5c01073 |
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