Article (Scientific journals)
Discovery and preliminary SARs of keto-indoles as novel indoleamine 2,3-dioxygenase (IDO) inhibitors.
Dolusic, Eduard; Larrieu, Pierre; Blanc, Sebastien et al.
2011In European Journal of Medicinal Chemistry, 46 (7), p. 3058-65
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Keywords :
Indoleamine 2,3-dioxygenase; Structuree activity relationships; Keto-indoles
Abstract :
[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.
Disciplines :
Oncology
Author, co-author :
Dolusic, Eduard
Larrieu, Pierre
Blanc, Sebastien
Sapunaric, Frédéric 
Pouyez, Jenny
Moineaux, Laurence
Colette, Delphine
Stroobant, Vincent
Pilotte, Luc
Colau, Didier
Ferain, Thierry
Fraser, Graeme;  Université de Liège - ULiège > Département des sciences de la vie > Macromolécules biologiques
Galleni, Moreno ;  Université de Liège - ULiège > Centre d'ingénierie des protéines
Masereel, Bernard
Van den Eynde, Benoit
Wouters, Johan
Frederick, Raphael
More authors (8 more) Less
Language :
English
Title :
Discovery and preliminary SARs of keto-indoles as novel indoleamine 2,3-dioxygenase (IDO) inhibitors.
Publication date :
2011
Journal title :
European Journal of Medicinal Chemistry
ISSN :
0223-5234
eISSN :
1768-3254
Publisher :
Elsevier, Netherlands
Volume :
46
Issue :
7
Pages :
3058-65
Peer reviewed :
Peer Reviewed verified by ORBi
Commentary :
Copyright (c) 2011 Elsevier Masson SAS. All rights reserved.
Available on ORBi :
since 31 May 2011

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