Discovery and Optimization Of Indole-pyridinyl-ethanones as Novel Inhibitors of Indoleamine-2,3-Dioxygenase (IDO), a Promising Target for Anti-Cancer Immunotherapy

Raphaël Frédérick, Sébastien Blanc, Pierre Larrieu, Laurence Moineaux, Delphine Colette, Graeme Fraser, Vincent Stroobant, Luc Pilotte, Didier Colau, Johan Wouters, Bernard Masereel, Benoît Van den Eynde, Eduard Dolusic

Research output: Contribution to conferencePoster

Abstract

Cancers and tumors regularly evade the immune surveillance system of the host employing several mechanisms. It was found previously that one mechanism resulting in tumoral immune resistance stems from the constitutive expression of indoleamine 2,3-dioxygenase (IDO) by tumor cells1
The present work is based on the recent discovery that a second enzyme in tryptophan catabolism, tryptophan 2,3-dioxygenase (TDO), is also unexpectedly expressed in many tumor cells.2,3
This work4 describes the design, synthesis, X-ray structure determination, enzyme inhibition, cellular assays, docking and solubility tests of indole-based TDO inhibitors of the general structure 1. This strategy is based on similar compounds reported as dual TDO/5-HT reuptake inhibitors.5
Original languageEnglish
PagesPC.281, 21st ISMC, Brussels, Belgium, September 5-9, 2010, Drugs of the Future, volume 35, issue suppl. A, pp. 181-182
Number of pages2
Publication statusPublished - 2010
EventEFMC-ISMC 2010 XXIst INTERNATIONAL SYMPOSIUM ON MEDICINAL CHEMISTRY - Bruxelles, Belgium
Duration: 5 Sep 2010 → …

Conference

ConferenceEFMC-ISMC 2010 XXIst INTERNATIONAL SYMPOSIUM ON MEDICINAL CHEMISTRY
CountryBelgium
CityBruxelles
Period5/09/10 → …

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