| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1393062 | European Journal of Medicinal Chemistry | 2011 | 8 Pages |
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.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Indoleamine 2,3-dioxygenase (IDO) involved in anticancer immunosuppression. ► Keto-indoles are novel IDO inhibitors. ► Substitution in the 5-position allows to enhance IDO inhibition. ► Keto-indoles act as uncompetitive inhibitors.
