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

Dolusic, Eduard;Larrieu, Pierre;Blanc, Sébastien;Sapunaric, Frédéric;Frédérick, Raphaël;et.al.
(2011) European Journal of Medicinal Chemistry — Vol. 46, n° 7, p. 3058-3065 (2011)

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Abstract
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.
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Dolusic, E., Larrieu, P., Blanc, S., Sapunaric, F., Pouyez, J., Moineaux, L., Colette, D., Stroobant, V., Pilotte, L., Colau, D., Ferain, T., Fraser, G., Galleni, M., Frère, J.-M., Masereel, B., Van den Eynde, B., Wouters, J., & Frédérick, R. (2011). Discovery and preliminary SARs of keto-indoles as novel indoleamine 2,3-dioxygenase (IDO) inhibitors. European Journal of Medicinal Chemistry, 46(7), 3058-3065. https://doi.org/10.1016/j.ejmech.2011.02.049 (Original work published 2011)