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

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

Open link

Publication date

January 2014

DOI

10.1039/c4dt00444b

Publisher

Royal Society of Chemistry (RSC)

ISSN

1477-9226

Journal

Dalton Transactions

Citation count (estimate)

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.6 page(s