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

doi:10.1039/C4DT00444B

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

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

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* Corresponding authors

^a School of Chemistry, The University of Sydney, Sydney, NSW 2006, Australia
E-mail: lou.rendina@sydney.edu.au

^b Department of Chemistry and Biomolecular Sciences, Macquarie University, Sydney, NSW 2109, Australia

^c Faculty of Pharmacy, The University of Sydney, Sydney, NSW 2006, Australia

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.

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

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