Reference : Discovery and preliminary SARs of keto-indoles as novel indoleamine 2,3-dioxygenase (...
Scientific journals : Article
Human health sciences : Oncology
http://hdl.handle.net/2268/92049
Discovery and preliminary SARs of keto-indoles as novel indoleamine 2,3-dioxygenase (IDO) inhibitors.
English
Dolusic, Eduard [> > > >]
Larrieu, Pierre [> > > >]
Blanc, Sebastien [> > > >]
Sapunaric, Frédéric mailto [> > > >]
Pouyez, Jenny [> > > >]
Moineaux, Laurence [> > > >]
Colette, Delphine [> > > >]
Stroobant, Vincent [> > > >]
Pilotte, Luc [> > > >]
Colau, Didier [> > > >]
Ferain, Thierry [> > > >]
Fraser, Graeme [Université de Liège - ULg > Département des sciences de la vie > Macromolécules biologiques]
Galleni, Moreno mailto [Université de Liège - ULg > > Centre d'ingénierie des protéines]
Frère, Jean-Marie mailto [> > > >]
Masereel, Bernard [> > > >]
Van den Eynde, Benoit [> > > >]
Wouters, Johan [> > > >]
Frederick, Raphael [ > > ]
2011
European journal of medicinal chemistry
46
7
3058-65
Yes (verified by ORBi)
International
0223-5234
1768-3254
France
[en] Indoleamine 2,3-dioxygenase ; Structuree activity relationships ; Keto-indoles
[en] 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.
Researchers ; Professionals ; Students
http://hdl.handle.net/2268/92049
10.1016/j.ejmech.2011.02.049
Copyright (c) 2011 Elsevier Masson SAS. All rights reserved.

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