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Issue 3, 2015
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Gold(i) thiotetrazolates as thioredoxin reductase inhibitors and antiproliferative agents

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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

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Supplementary files

Article information


Submitted
08 Oct 2014
Accepted
04 Nov 2014
First published
21 Nov 2014

This article is Open Access

Dalton Trans., 2015,44, 1161-1169
Article type
Paper
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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