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Bioorg Med Chem. 2011 Feb 15;19(4):1550-61. doi: 10.1016/j.bmc.2010.12.032. Epub 2010 Dec 16.

Indol-2-yl ethanones as novel indoleamine 2,3-dioxygenase (IDO) inhibitors.

Author information

  • 1Drug design and Discovery Center, University of Namur, 61 Rue de Bruxelles, 5000 Namur, Belgium.

Erratum in

  • Bioorg Med Chem. 2011 May 1;19(9):3029. Galeni, Moreno [corrected to Galleni, Moreno].


Indoleamine 2,3-dioxygenase (IDO) is a heme dioxygenase which has been shown to be involved in the pathological immune escape of diseases such as cancer. The synthesis and structure-activity relationships (SAR) of a novel series of IDO inhibitors based on the indol-2-yl ethanone scaffold is described. In vitro and in vivo biological activities have been evaluated, leading to compounds with IC(50) values in the micromolar range in both tests. Introduction of small substituents in the 5- and 6-positions of the indole ring, indole N-methylation and variations of the aromatic side chain are all well tolerated. An iron coordinating group on the linker is a prerequisite for biological activity, thus corroborating the virtual screening results.

Copyright © 2010 Elsevier Ltd. All rights reserved.

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