Physiological and pathological functions of thioredoxine reductase (TrxR) system in cellular processes have been extensively investigated. Available evidences approve that dysregulation of TrxR results in various human diseases, especially cancer.

An increasing number of TrxR inhibitors which are in clinical trials for the treatment of different types of cancers has been reported so far. However, construction of the specific inhibitors of TrxR over other related enzymes (e.g. glutathione reductase) remains a challenge.

One of our research direction, is synthesis of small, structurally diverse products to define a new and selective class of Trx inhibitors. Herein, we present a library of natural small compounds (including sanatmarine, coumarine and asparagusic acid derivatives) possessing a potential Michael acceptor moiety and disulfide bond, respectively. The preliminary biological activity results proved the obtained library to be specific inhibitors although the mechanism of action and stability is still under investigation.