Issue 3, 2015

Gold(i) thiotetrazolates as thioredoxin reductase inhibitors and antiproliferative agents

Abstract

Gold(I) complexes with phosphane and thiotetrazolate ligands were prepared and investigated as a new type of bioactive gold metallodrugs. The complexes triggered very efficient inhibition of the enzyme thioredoxin reductase (TrxR), which is an important molecular target for gold species. Strong cytotoxic effects were observed in MDA-MB-231 breast adenocarcinoma and HT-29 colon carcinoma cells, and the complexes also caused strong effects in vincristine resistant Nalm-6 leukemia cells. Cellular uptake studies showed elevated cellular gold levels for complexes containing a triphenylphosphane ligand, whereas trifurylphosphane analogues accumulated at significantly lower cellular concentrations.

Graphical abstract: Gold(i) thiotetrazolates as thioredoxin reductase inhibitors and antiproliferative agents

Supplementary files

Article information

Article type
Paper
Submitted
08 Oct 2014
Accepted
04 Nov 2014
First published
21 Nov 2014
This article is Open Access
Creative Commons BY license

Dalton Trans., 2015,44, 1161-1169

Author version available

Gold(I) thiotetrazolates as thioredoxin reductase inhibitors and antiproliferative agents

T. V. Serebryanskaya, A. S. Lyakhov, L. S. Ivashkevich, J. Schur, C. Frias, A. Prokop and I. Ott, Dalton Trans., 2015, 44, 1161 DOI: 10.1039/C4DT03105A

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