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

Dalton Transactions Pub Date: 2014-04-22 DOI: 10.1039/C4DT00444B

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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