Development of a series of novel o-phenylenediamine-based indoleamine 2, 3-dioxygenase 1 (IDO1) inhibitors. Issue 4 (15th February 2018)

• Record Type: Journal Article
• Authors: Williams, David K.; Markwalder, Jay A.; Balog, Aaron J.; Chen, Bin; Chen, Libing; Donnell, Jennifer; Haque, Lauren; Hart, Amy C.; Mandal, Sunil K.; Nation, Andrew; Shan, Weifang; Vite, Gregory D.; Covello, Kelly; Hunt, John T.; Jure-Kunkel, Maria N.; Seitz, Steven P.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 28:Issue 4(2018)
• Page Start: 732
• Page End: 736
• Publication Date: 2018-02-15
• Subjects: Indoleamine 2, 3-dioxygenase -- IDO -- IDO1 -- Immuno-oncology -- Kynurenine; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2018.01.010
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: A novel series of o -phenylenediamine-based inhibitors of indoleamine 2, 3-dioxygenase (IDO) has been identified. Compound 19 demonstrated significant potency in the HeLa human cervical cancer IDO1 assay. Abstract: A novel series of o -phenylenediamine-based inhibitors of indoleamine 2, 3-dioxygenase (IDO) has been identified. IDO is a heme-containing enzyme, overexpressed in the tumor microenvironment of many cancers, which can contribute to the suppression of the host immune system. Synthetic modifications to a previously described diarylether series resulted in an additional degree of molecular diversity which was exploited to afford compounds that demonstrated significant potency in the HeLa human cervical cancer IDO1 assay. .