A complex bearing TSPO PIGA ligand coordinated to the [Au(PEt₃)]⁺ pharmacophore is highly cytotoxic against ovarian cancer cells.

ABSTRACT: Auranofin ([1-(thio-κS)-β-D-glucopyranose-2,3,4,6-tetraacetato](triethylphosphine)-gold) is a leading gold-based drug clinically used to treat arthritis. In the last years, it entered various drug reprofiling programs, and it has been found promising against various forms of tumor, including ovarian cancer. Evidence showed as its antiproliferative profile mainly depends on the inhibition of thioredoxin reductase (TrxR), being this mitochondrial system its main target. In this context, we report here the synthesis and biological evaluation of a novel complex designed as auranofin analogue obtained through the conjugation of a phenylindolylglyoxylamide ligand (which belongs to the so-called PIGA TSPO ligand family) with the auranofin-derived cationic fragment [Au(PEt₃)]⁺

SUBMITTER: Chiaverini L 

PROVIDER: S-EPMC10545567 | biostudies-literature | 2023 Oct

REPOSITORIES: biostudies-literature