2. Academic Validation
  3. Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model

Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model

  • J Med Chem. 2009 Dec 10;52(23):7364-7. doi: 10.1021/jm900518f.
Eddy W Yue 1,  Brent Douty,  Brian Wayland,  Michael Bower,  Xiangdong Liu,  Lynn Leffet,  Qian Wang,  Kevin J Bowman,  Michael J Hansbury,  Changnian Liu,  Min Wei,  Yanlong Li,  Richard Wynn,  Timothy C Burn,  Holly K Koblish,  Jordan S Fridman,  Brian Metcalf,  Peggy A Scherle,  Andrew P Combs
Affiliations

Affiliation

  • 1 Incyte Corporation, Experimental Station, Route 141 and Henry Clay Road, Wilmington, Delaware 19880, USA.
PMID: 19507862 DOI: 10.1021/jm900518f
Abstract

A hydroxyamidine chemotype has been discovered as a key pharmacophore in novel inhibitors of indoleamine 2,3-dioxygenase (IDO). Optimization led to the identification of 5l, which is a potent (HeLa IC(50) = 19 nM) competitive inhibitor of IDO. Testing of 5l in mice demonstrated pharmacodynamic inhibition of IDO, as measured by decreased kynurenine levels (>50%) in plasma and dose dependent efficacy in mice bearing GM-CSF-secreting B16 melanoma tumors.

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