Discovery and preliminary SARs of keto-indoles as novel indoleamine 2,3-dioxygenase (IDO) inhibitors

E. Dolušić, P. Larrieu, S. Blanc, F. Sapunaric, J. Pouyez, L. Moineaux, D. Colette, V. Stroobant, L. Pilotte, D. Colau, Thierry Ferain, G. Fraser, M. Galleni, Jean-Marie Frère, B. Masereel, B. Van Den Eynde, J. Wouters, R. Frédérick

Research output: Contribution to journalArticlepeer-review


Indoleamine 2,3-dioxygenase (IDO) is an important new therapeutic target for the treatment of cancer. With the aim of discovering novel IDO inhibitors, a virtual screen was undertaken and led to the discovery of the keto-indole derivative 1a endowed with an inhibitory potency in the micromolar range. Detailed kinetics were performed and revealed an uncompetitive inhibition profile. Preliminary SARs were drawn in this series and corroborated the putative binding orientation as suggested by docking. © 2011 Elsevier Masson SAS. All rights reserved.
Original languageEnglish
Pages (from-to)3058-3065
Number of pages8
JournalEuropean Journal of Medicinal Chemistry
Issue number7
Publication statusPublished - 2011


  • enzyme inhibitors
  • keto-indoles
  • Structure-activity relationships
  • Structure-based drug discovery
  • IDO
  • Indoleamine 2 3-dioxygenase


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