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Re(I) and Re(I)/Au(I) complexes for cell imaging and therapy applications

AuthorsLuengo, Andrés; Fernández-Moreira, Vanesa ; Marzo, Isabel; Gimeno, M. Concepción
Gold (I)
Drug design
NHC carbenes
Cell imaging
Issue Date2016
Citation6th EuCheMS (2016)
AbstractCationic rhenium(I) complexes bearing a diimine ligand are known to exhibit excellent luminescent properties as well as low cytotoxicity, making them suitable for use in cell imaging. Those compounds usually accumulate in mitochondria enabling its visualization through fluorescence microscopy, but also its use as localization vectors for ligands chemically linked to Re. The substitution of the diimine for a pyridyl-N-heterocyclic carbene (NHC) ligand as N^C chelate could result in a new biodistribution pattern and, consequently, the visualization and targeting of different organelles. These compounds have not been studied yet for cell imaging applications. Additionally, as NHC ligands are stronger donor ligands than pyridyl derivatives, higher energy LUMO orbitals as well as blue-shifted emissions should be observed, opening the door to the design of new Re compounds for OLEDs. A series of new Re(I) derivatives have been synthetized starting from the fac-[Re(N^C)(CO)3Cl] precursor through the activated intermediate fac-[Re(N^C)(CO)3NCCH3]+ (Scheme 1). The obtained compounds showed higher excitation energy compared to bipy analogue derivatives, and poorer luminescence because of an increment of the flexibility of the chelate ligand bearing the N^C moiety. Additionally, few ligands were also functionalized with alkynyl-gold units in order to increase cytotoxic activity of the products (Scheme 2). The formation of bimetallic complexes, containing a luminescent Re(I) fragment with a cytotoxic Au(I) moiety may allow understanding the mechanism of action of these drugs. Cytotoxicity and biodistribution measurements are in process.
DescriptionResumen del póster presentado al 6th EuCheMS Chemistry Congress, celebrado en Sevilla (España) del 11 al 15 de septiembre de 2016.
Appears in Collections:(ISQCH) Comunicaciones congresos
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