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

20 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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TY - JOUR

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.

UR - https://www.scopus.com/pages/publications/84903464291

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

Abstract

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