| Literature DB >> 24752804 |
Christopher J D Austin1, Jan Kahlert, Fatiah Issa, John H Reed, Jason R Smith, Joseph A Ioppolo, Jennifer A Ong, Joanne F Jamie, David Hibbs, Louis M Rendina.
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.Entities:
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Year: 2014 PMID： 24752804 DOI： 10.1039/c4dt00444b
Source DB: PubMed Journal: Dalton Trans ISSN： 1477-9226 Impact factor: 4.390