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

Overview

Journal Angew Chem Int Ed Engl

Specialty Chemistry

Date 2020 Jul 8

PMID 32633820

Citations 6

Authors

Federica Guarra

Alessio Terenzi

Christine Pirker

Rossana Passannante

Dina Baier

Ennio Zangrando

Vanessa Gomez-Vallejo

Tarita Biver

Chiara Gabbiani

Walter Berger

Jordi Llop

Luca Salassa

Affiliations

Soon will be listed here.

Abstract

Au 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 -NHC complexes by direct oxidation with radioactive [ I]I 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 -to-Au reduction to achieve full anticancer activity, in vivo studies reveal that a fraction of the Au -NHC prodrug is not immediately reduced after administration but able to reach the major organs before metabolic activation.

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