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124 I Radiolabeling of a Au III ‐NHC Complex for In Vivo Biodistribution Studies
Author(s) -
Guarra Federica,
Terenzi Alessio,
Pirker Christine,
Passannante Rossana,
Baier Dina,
Zangrando Ennio,
GómezVallejo Vanessa,
Biver Tarita,
Gabbiani Chiara,
Berger Walter,
Llop Jordi,
Salassa Luca
Publication year - 2020
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.202008046
Subject(s) - biodistribution , in vivo , chemistry , prodrug , radiochemistry , in vitro , combinatorial chemistry , biochemistry , biology , microbiology and biotechnology
Au III 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 Au III ‐NHC complexes by direct oxidation with radioactive [ 124 I]I 2 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 Au III ‐to‐Au I reduction to achieve full anticancer activity, in vivo studies reveal that a fraction of the Au III ‐NHC prodrug is not immediately reduced after administration but able to reach the major organs before metabolic activation.