Projects per year
Abstract
We set out to develop new, improved TDO inhibitors using as the starting point the only (unoptimized) series previously known in the literature.3
Herein, we describe the syntheses and structure-activity studies around a series of 3-alkenyl indoles and their derivatives.4 The TDO inhibitory potency was evaluated and rationalized by molecular modeling studies, while solubility, stability and oral bioavailability were determined for selected compounds. The most promising candidate was evaluated in a preclinical model in mice where, upon systemic treatment, it indeed reversed TDO-mediated tumoral immune resistance.5
Original language | English |
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Pages | Book of Abstracts, Heterocycles in Bio-organic Chemistry, Riga, Latvia, 27 - 30 May 2013, PO129 |
Number of pages | 1 |
Publication status | Published - 27 May 2013 |
Event | Heterocycles in Bio-organic Chemistry - Riga, Latvia Duration: 27 May 2013 → 30 May 2013 |
Conference
Conference | Heterocycles in Bio-organic Chemistry |
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Country | Latvia |
City | Riga |
Period | 27/05/13 → 30/05/13 |
Fingerprint Dive into the research topics of '3-ALKENYL INDOLES AS TRYPTOPHAN 2,3-DIOXYGENASE INHIBITORS FOR THE ENHANCEMENT OF CANCER IMMUNOTHERAPY'. Together they form a unique fingerprint.
Projects
- 2 Finished
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Design, synthesis and study of enzyme modulators implicated in tryptophan metabolism and particularly in the kynurenin pathway
FREDERICK, R.
1/10/07 → 30/09/10
Project: Research
Equipment
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Physical Chemistry and characterization(PC2)
Johan Wouters (Manager) & Carmela Aprile (Manager)
Technological Platform Physical Chemistry and characterizationFacility/equipment: Technological Platform
Activities
- 2 Participation in conference
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Heterocycles in Bio-organic Chemistry
Eduard Dolusic (Poster)
27 May 2013Activity: Participating in or organising an event types › Participation in conference
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EFMC-ISMC 2010 XXIst INTERNATIONAL SYMPOSIUM ON MEDICINAL CHEMISTRY
Eduard Dolusic (Poster)
5 Sep 2010 → 9 Sep 2010Activity: Participating in or organising an event types › Participation in conference
Press / Media
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Mladi Ogulinac u ekipi koja je na tragu lijeka protiv raka
24/02/12
1 item of Media coverage
Press/Media: Other
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Broadening TDO's base
Eduard Dolusic, Raphaël Frederick, Bernard Masereel & Johan Wouters
23/02/12
1 item of Media coverage
Press/Media: Expert Comment
Student Theses
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Caractérisation enzymatique et structurale d'inhibiteurs indoliques de la tryptophane 2,3-dioxygénase.: Mémoire présenté pour l'obtention du grade académique de Master en Chimie "Chimie du Vivant et des Nanomatériaux" : Finalité Spécialisée.
Author: Molle, N., 2012Supervisor: Wouters, J. (Supervisor), Dolusic, E. (Jury), Moineaux, L. (Jury), Fonder, G. (Jury) & Leherte, L. (Jury)
Student thesis: Master types › Master in Chemistry