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

• Main Authors: Koh, Wei Xiang, Coppo, Lucia, Ganguly, Rakesh, Holmgren, Arne, Leong, Weng Kee
• Other Authors: School of Physical and Mathematical Sciences
• Format: Article
• Language: English
• Published: 2022
• Subjects: Science::Chemistry; Ebselen; Metallocenyl
• Online Access: https://hdl.handle.net/10356/159768
• Institution: Nanyang Technological University

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 natura...