Metallocenyl derivatives of ebselen are selective and competitive inhibitors of thioredoxin reductase

Abstract

Ferrocenyl and ruthenocenyl derivatives of ebselen are found to be competitive inhibitors of mammalian TrxR, with IC50 of 4.2 ± 0.3 and 2.5 ± 0.3 µM, respectively. The inhibition of TrxR is selective over GR, and in the presence of excess GSH. They exhibit lower Km values than ebselen and the natural substrate, Trx.