Study of the effect of the chromophore and nuclearity on the aggregation and potential biological activity of gold(I) alkynyl complexes

• Published in: Inorganica Chimica Acta Vol. 446; pp. 189 - 197
• Main Authors: Gavara, Raquel, Aguiló, Elisabet, Schur, Julia, Llorca, Jordi, Ott, Ingo, Rodríguez, Laura
• Format: Journal Article Publication
• Language: English
• Published: Elsevier B.V 01-05-2016
• Subjects: Alkynyl; Antitumor-activity; Carbene complexes; Ciències de la salut; Cytotoxicity; derivatives; Drugs; Enginyeria química; Farmacologia; Farmacologia molecular; Gold; In-vitro; Inhibition; Luminescence; Mechanisms; Medicina; Medicina interna; Molecular pharmacology; Química inorgànica; Thioredoxin reductase; Àrees temàtiques de la UPC; Gold; Cytotoxicity; Alkynyl; Thioredoxin reductase; Luminescence
• ISSN: 0020-1693; 1873-3255
• DOI: 10.1016/j.ica.2016.03.012

The synthesis, characterization, aggregation and emissive properties of four organometallic gold(I) complexes containing different water soluble phosphanes and chromophoric units is here reported. Biological activity of the complexes showed very low effects against tumor cell growth but an inhibitory potency against thioredoxin reductase (TrxR). [Display omitted]
•Synthesis and characterization of four organometallic gold(I) complexes.•Complexes with different water soluble phosphanes and chromophoric units.•Study of the emissive and aggregation properties.•Biological studies show low cytotoxicity but good TrxR inhibition.
The synthesis and characterization of four organometallic gold(I) complexes containing different water soluble phosphanes (TPPTS, PTA and DAPTA) and chromophoric units (4-pyridylethynyl and propargyloxycoumarin) is here reported. The analysis of their absorption and emission spectra led us to attribute their luminescent behavior to the chromophoric organic ligands. Moreover, the presence of the gold(I) metal atom has been observed to be the responsible of an efficient intersystem crossing process responsible for the observed phosphorescence emission. Broad emission bands are observed in most cases due to the formation of organized aggregates in solution in agreement with microscopic characterization.
Biological activity of the complexes showed very low effects against tumor cell growth but an inhibitory potency against thioredoxin reductase (TrxR). The missing/low cytotoxic effects could be related to a low bioavailability as determined by atomic absorption spectroscopy.