The first indoleamine-2,3-dioxygenase-1 (IDO1) inhibitors containing carborane

Christopher J D Austin, Jan Kahlert, Fatiah Issa, John H. Reed, Jason R. Smith, Joseph A. Ioppolo, Jennifer A. Ong, Joanne F. Jamie, David Hibbs, Louis M. Rendina*

*Corresponding author for this work

Research output: Contribution to journalArticle

15 Citations (Scopus)

Abstract

Indoleamine-2,3-dioxygenase-1 (IDO1) is a critical immunoregulatory enzyme responsible for the metabolism of tryptophan during inflammation and disease. Based upon a pyranonaphthoquinone framework, the first examples of indoleamine-2,3-dioxygenase-1 (IDO1) inhibitors containing a carborane cage are reported. The novel closo-1,2-carboranyl-N-pyranonaphthoquinone derivatives display low μM binding affinity for the human recombinant enzyme, with IC50 values ranging from 0.78 to 1.77 μM.

Original languageEnglish
Pages (from-to)10719-10724
Number of pages6
JournalDalton Transactions
Volume43
Issue number28
DOIs
Publication statusPublished - 28 Jul 2014

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    Austin, C. J. D., Kahlert, J., Issa, F., Reed, J. H., Smith, J. R., Ioppolo, J. A., ... Rendina, L. M. (2014). The first indoleamine-2,3-dioxygenase-1 (IDO1) inhibitors containing carborane. Dalton Transactions, 43(28), 10719-10724. https://doi.org/10.1039/c4dt00444b