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Bioorg Med Chem Lett. 2017 Feb 1;27(3):582-585. doi: 10.1016/j.bmcl.2016.12.015. Epub 2016 Dec 7.

Identification and optimization of a novel series of indoleamine 2,3-dioxygenase inhibitors.

Author information

1
Oncology Chemistry, Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-5400, United States. Electronic address: jay.markwalder@bms.com.
2
Oncology Chemistry, Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-5400, United States.
3
Mechanistic Biochemistry, Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-5400, United States.
4
Lead Discovery & Optimization, Bristol-Myers Squibb Research and Development, Wallingford, CT 06492, United States.
5
Oncology Biology, Bristol-Myers Squibb Research and Development, Princeton, NJ 08543-5400, United States.

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.

KEYWORDS:

IDO; Immuno-oncology; Indoleamine 2,3-dioxygenase; Kynurenine

PMID:
28003141
DOI:
10.1016/j.bmcl.2016.12.015
[Indexed for MEDLINE]

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