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

Journal article


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 and Rendina, Louis M.. (2014). The first indoleamine-2,3-dioxygenase-1 (IDO1) inhibitors containing carborane. Dalton Transactions. 43(28), pp. 10719-10724. https://doi.org/10.1039/c4dt00444b
AuthorsAustin, Christopher J. D., Kahlert, Jan, Issa, Fatiah, Reed, John H., Smith, Jason R., Ioppolo, Joseph A., Ong, Jennifer A., Jamie, Joanne F., Hibbs, David and Rendina, Louis M.
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.

Year2014
JournalDalton Transactions
Journal citation43 (28), pp. 10719-10724
PublisherRoyal Society of Chemistry
ISSN1477-9226
Digital Object Identifier (DOI)https://doi.org/10.1039/c4dt00444b
Scopus EID2-s2.0-84903464291
Open accessPublished as green open access
Research or scholarlyResearch
Page range10719-10724
Author's accepted manuscript
License
All rights reserved
File Access Level
Open
Publisher's version
License
All rights reserved
File Access Level
Controlled
Output statusPublished
Publication dates
Online22 Apr 2014
Publication process dates
Accepted03 Apr 2014
Deposited28 Oct 2021
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Kahlert, Jan U., Austin, Christopher J. D., Hall, Andrew J., Rawal, Aditya, Hook, James M., Rendina, Louis M. and Choucair, Mohammad. (2016). Site-specific synthesis of a hybrid boron-graphene salt. Chemical Communications. 52(6), pp. 1290-1292. https://doi.org/10.1039/c5cc07611k