Identification and optimization of a novel series of indoleamine 2, 3-dioxygenase inhibitors. Issue 3 (1st February 2017)

• Record Type: Journal Article
• Authors: Markwalder, Jay A.; Seitz, Steven P.; Blat, Yuval; Elkin, Lisa; Hunt, John T.; Pabalan, Jonathan G.; Jure-Kunkel, Maria N.; Vite, Gregory D.; Covello, Kelly
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 3(2017)
• Page Start: 582
• Page End: 585
• Publication Date: 2017-02-01
• Subjects: IDO -- Kynurenine -- Indoleamine 2, 3-dioxygenase -- Immuno-oncology; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.12.015
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: The discovery of a series of structurally-novel biaryl urea IDO inhibitors is described. Optimization of a micromolar hit through iterative cycles of synthesis and screening in an assay measuring IDO-mediated intracellular conversion of tryptophan to kynurenine led to potent inhibitors with favorable selectivity and metabolic stability profiles.