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Issue 28, 2014
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The first indoleamine-2,3-dioxygenase-1 (IDO1) inhibitors containing carborane

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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.

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

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Publication details

The article was received on 12 Feb 2014, accepted on 03 Apr 2014 and first published on 22 Apr 2014


Article type: Paper
DOI: 10.1039/C4DT00444B
Author version available: Download Author version (PDF)
Citation: Dalton Trans., 2014,43, 10719-10724
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    The first indoleamine-2,3-dioxygenase-1 (IDO1) inhibitors containing carborane

    C. J. D. Austin, J. Kahlert, F. Issa, J. H. Reed, J. R. Smith, J. A. Ioppolo, J. A. Ong, J. F. Jamie, D. Hibbs and L. M. Rendina, Dalton Trans., 2014, 43, 10719
    DOI: 10.1039/C4DT00444B

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