Reference : Indol-2-yl ethanones as novel indoleamine 2,3-dioxygenase (IDO) inhibitors.
Scientific journals : Article
Human health sciences : Oncology
http://hdl.handle.net/2268/94805
Indol-2-yl ethanones as novel indoleamine 2,3-dioxygenase (IDO) inhibitors.
English
Dolusic, Eduard [Facultés Universitaires Notre-Dame de la Paix - Namur - FUNDP > > > >]
Larrieu, Pierre [Université Catholique de Louvain - UCL > > > >]
Blanc, Sébastien [Euroscreen > > > >]
Sapunaric, Frédéric mailto [Université de Liège - ULg > > Centre d'ingénierie des protéines >]
Norberg, Bernadette [Facultés Universitaires Notre-Dame de la Paix - Namur - FUNDP > > > >]
Moineaux, Laurence [Facultés Universitaires Notre-Dame de la Paix - Namur - FUNDP > > > >]
Colette, Delphine [Facultés Universitaires Notre-Dame de la Paix - Namur - FUNDP > > > >]
Stroobant, Vincent [Université Catholique de Louvain - UCL > > > >]
Pilotte, Luc [Université Catholique de Louvain - UCL > > > >]
Colau, Didier [Université Catholique de Louvain - UCL > > > >]
Ferain, Thierry [Euroscreen > > > >]
Fraser, Graeme [Euroscreen > > > >]
Galleni, Moreno mailto [Université de Liège - ULg > > Centre d'ingénierie des protéines >]
Frère, Jean-Marie mailto [Université de Liège - ULg > > Centre d'ingénierie des protéines >]
Masereel, Bernard [Facultés Universitaires Notre-Dame de la Paix - Namur - FUNDP > > > >]
Van den Eynde, Benoit [Université Catholique de Louvain - UCL > > > >]
Wouters, Johan [Facultés Universitaires Notre-Dame de la Paix - Namur - FUNDP > > > >]
Frederick, Raphael [Facultés Universitaires Notre-Dame de la Paix - Namur - FUNDP > > > >]
2011
Bioorganic & Medicinal Chemistry
Elsevier Science
19
4
1550-61
Yes (verified by ORBi)
International
0968-0896
1464-3391
Oxford
United Kingdom
[en] Catalytic Domain ; Cell Line ; Ethane/chemistry ; Humans ; Indoleamine-Pyrrole 2,3,-Dioxygenase/antagonists & inhibitors/chemistry ; Indoles/chemistry/pharmacology ; Models, Molecular ; Protein Interaction Domains and Motifs ; Structure-Activity Relationship
[en] 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.
http://hdl.handle.net/2268/94805
10.1016/j.bmc.2010.12.032
Copyright (c) 2010 Elsevier Ltd. All rights reserved.

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