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

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

18 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
Externally published	Yes

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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",

volume = "43",

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

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AN - SCOPUS:84903464291

SN - 1477-9226

VL - 43

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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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