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

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Dolusic, Eduard [FUNDP] Larrieu, Pierre [UCL] Blanc, Sébastien [Euroscreen SA] Sapunaric, Frédéric [ULg] Pouyez, Jenny [FUNDP] Moineaux, Laurence [FUNDP] Stroobant, Vincent [UCL] Pilotte, Luc [UCL] Colau, Didier [UCL] Masereel, Bernard [FUNDP] Van den Eynde, Benoît [UCL] Wouters, Johan [FUNDP] Frédérick, Raphaël [UCL]

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.

Document type Article de périodique (Journal article)
Access type Accès restreint
Publication date 2011
Language Anglais
Journal information "European Journal of Medicinal Chemistry" - Vol. 46, no. 7, p. 3058-3065 (2011)
Peer reviewed yes
Publisher Elsevier Masson ((France) Issy les Moulineaux)
issn 0223-5234
e-issn 1768-3254
Publication status Publié
Affiliations FUNDP - Autre
Euroscreen SA - Gosselies, Belgique
ULg - Centre d’Ingénierie des Protéines
UCL - SSS/DDUV - Institut de Duve
UCL - SSS/LDRI - Louvain Drug Research Institute
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Bibliographic reference Dolusic, Eduard ; Larrieu, Pierre ; Blanc, Sébastien ; Sapunaric, Frédéric ; Pouyez, Jenny ; et. al. Discovery and preliminary SARs of keto-indoles as novel indoleamine 2,3-dioxygenase (IDO) inhibitors. In: European Journal of Medicinal Chemistry, Vol. 46, no. 7, p. 3058-3065 (2011)
Permanent URL http://hdl.handle.net/2078.1/106226