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- Title
A Gold(III) Pincer Ligand Scaffold for the Synthesis of Binuclear and Bioconjugated Complexes: Synthesis and Anticancer Potential.
- Authors
Bochmann, Manfred; Bertrand, Benoît; O'Connell, Maria A.; Waller, Zoë A. E.
- Abstract
Abstract: Cyclometalated (C^N^C)AuIII complexes bearing functionalized N‐heterocyclic carbene (NHC) ligands provide a high‐yielding, modular route to bioconjugated and binuclear complexes. This methodology has been applied to the synthesis of bioconjugated complexes presenting biotin and 17α‐ethynylestradiol vectors, as well as to the synthesis of bimetallic AuIII/AuI complexes. The in vitro antiproliferative activities of these compounds against various cancer cells lines depend on the linker length, with the longer linker being the most potent. The estradiol conjugate <bold>AuC6Estra</bold> proved to be more toxic against the estrogen receptor positive (ER+) cancer cells than against the ER− cancer cells and non‐cancer cells. The bimetallic complex <bold>AuC6Au</bold> was more selective for breast cancer cells with respect to a healthy cell standard than the monometallic complex <bold>AuNHC</bold>. The metal uptake study on cells expressing or not biotin and estrogen receptors revealed an improved and targeted delivery of gold for both the bioconjugated complexes <bold>AuC6Biot</bold> and <bold>AuC6Estra</bold> compared to the non‐vectorised analogue <bold>AuNHC</bold>. The investigations of the interaction of the bioconjugates and bimetallic complexes with human telomeric G‐quadruplex DNA using FRET‐melting techniques revealed a reduced ability to stabilize this DNA structure with respect to the non‐vectorised analogue <bold>AuNHC</bold>.
- Subjects
ANTINEOPLASTIC agents; METAL carbenes; BIOTIN; ESTROGEN receptors; BIMETALLIC catalysts
- Publication
Chemistry - A European Journal, 2018, Vol 24, Issue 14, p3613
- ISSN
0947-6539
- Publication type
Article
- DOI
10.1002/chem.201705902