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

Eduard Dolušić, Pierre Larrieu, Sébastien Blanc, Frédéric Sapunaric, Bernadette Norberg, Laurence Moineaux, Delphine Colette, Vincent Stroobant, Luc Pilotte, Didier Colau, Thierry Ferain, Graeme Fraser, Moreno Galeni, Jean Marie Frre, Bernard Masereel, Benoît Van Den Eynde, Johan Wouters, Raphaël Frédérick

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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. © 2011 Elsevier Ltd. All rights reserved.

Original languageEnglish
Pages (from-to)1550-1561
Number of pages12
JournalBioorganic and Medicinal Chemistry
Issue number4
Publication statusPublished - 15 Feb 2011
EventJFB 2011. - Liege, Belgium
Duration: 19 May 2011 → …


  • Anticancer
  • IDO
  • Immunotherapy
  • Indoleamine 2,3-dioxygenase


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