The first indoleamine-2,3-dioxygenase-1 (IDO1) inhibitors containing carborane
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Open Access
Type
ArticleAuthor/s
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.
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.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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Date
2014-04-22Publisher
Royal Society of ChemistryLicence
OtherFaculty/School
Faculty of Science, School of ChemistryCitation
Dalton Trans., 2014,43, 10719-10724Share