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, 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

Faculty of Science and Engineering

Research output: Contribution to journal › Article › peer-review

19 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 language	English
Pages (from-to)	10719-10724
Number of pages	6
Journal	Dalton Transactions
Volume	43
Issue number	28
DOIs	https://doi.org/10.1039/c4dt00444b
Publication status	Published - 28 Jul 2014

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

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.",

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

year = "2014",

month = jul,

day = "28",

doi = "10.1039/c4dt00444b",

language = "English",

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pages = "10719--10724",

journal = "Dalton Transactions",

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T1 - The first indoleamine-2,3-dioxygenase-1 (IDO1) inhibitors containing carborane

AU - Austin, Christopher J D

AU - Kahlert, Jan

AU - Issa, Fatiah

AU - Reed, John H.

AU - Smith, Jason R.

AU - Ioppolo, Joseph A.

AU - Ong, Jennifer A.

AU - Jamie, Joanne F.

AU - Hibbs, David

AU - Rendina, Louis M.

PY - 2014/7/28

Y1 - 2014/7/28

N2 - 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.

AB - 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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U2 - 10.1039/c4dt00444b

DO - 10.1039/c4dt00444b

M3 - Article

C2 - 24752804

AN - SCOPUS:84903464291

SN - 1477-9226

VL - 43

SP - 10719

EP - 10724

JO - Dalton Transactions

JF - Dalton Transactions

IS - 28

ER -

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

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