Research output per year
Research output per year
Eduard Dolušić, Pierre Larrieu, Sébastien Blanc, Frédéric Sapunaric, Bernadette Norberg, Laurence Moineaux, Delphine Colette, Vincent Stroobant, Luc Pilotte, Didier Colau, Thierry Ferain, Graeme Fraser, Moreno Galeni, Jean Marie Frre, Bernard Masereel, Benoît Van Den Eynde, Johan Wouters, Raphaël Frédérick
Research output: Contribution to journal › Article › peer-review
Indoleamine 2,3-dioxygenase (IDO) is a heme dioxygenase which has been shown to be involved in the pathological immune escape of diseases such as cancer. The synthesis and structure-activity relationships (SAR) of a novel series of IDO inhibitors based on the indol-2-yl ethanone scaffold is described. In vitro and in vivo biological activities have been evaluated, leading to compounds with IC 50 values in the micromolar range in both tests. Introduction of small substituents in the 5- and 6-positions of the indole ring, indole N-methylation and variations of the aromatic side chain are all well tolerated. An iron coordinating group on the linker is a prerequisite for biological activity, thus corroborating the virtual screening results. © 2011 Elsevier Ltd. All rights reserved.
Original language | English |
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Pages (from-to) | 1550-1561 |
Number of pages | 12 |
Journal | Bioorganic & medicinal chemistry |
Volume | 19 |
Issue number | 4 |
DOIs | |
Publication status | Published - 15 Feb 2011 |
Event | JFB 2011. - Liege, Belgium Duration: 19 May 2011 → … |
Research output: Contribution to journal › Literature review › peer-review
Research output: Contribution to journal › Article › peer-review
Research output: Contribution to journal › Article › peer-review
Masereel, B. (PI), Wouters, J. (PI), Dolušić, E. (Researcher), FREDERICK, R. (Researcher), POUYEZ, J. (Researcher), Van den Eynde, B. J. (CoI), Frère, J.-M. (CoI), Moser, M. (CoI), Jean-Marie, B. (CoI), Combalbert, J. (PI) & Stephenne, J. (CoI)
1/04/08 → 31/03/12
Project: Research
Wouters, J. (Manager), Aprile, C. (Manager) & Fusaro, L. (Manager)
Technological Platform Physical Chemistry and characterizationFacility/equipment: Technological Platform
Dolusic, E. (Poster)
Activity: Participating in or organising an event types › Participation in conference
Dolusic, E. (Speaker)
Activity: Participating in or organising an event types › Participation in conference
Dolusic, E. (Poster)
Activity: Participating in or organising an event types › Participation in conference
Dolusic, E. (Contributor), Larrieu, P. (Contributor), Blanc, S. (Contributor), Sapunaric, F. (Contributor), Norberg, B. (Contributor), Moineaux, L. (Contributor), Colette, D. (Contributor), Stroobant, V. (Contributor), Pilotte, L. (Contributor), Colau, D. (Contributor), Ferain, T. (Contributor), Fraser, G. (Contributor), Galeni, M. (Contributor), Frere, J.-M. (Contributor), Masereel, B. (Contributor), Benoit, V. D. E. (Contributor), Wouters, J. (Contributor) & Frederick, R. (Contributor), Cambridge Crystallographic Data Centre, 1 Jan 2011
DOI: 10.5517/ccvnpgm, http://www.ccdc.cam.ac.uk/services/structure_request?id=doi:10.5517/ccvnpgm&sid=DataCite
Dataset
Dolusic, E. (Contributor), Larrieu, P. (Contributor), Blanc, S. (Contributor), Sapunaric, F. (Contributor), Norberg, B. (Contributor), Moineaux, L. (Contributor), Colette, D. (Contributor), Stroobant, V. (Contributor), Pilotte, L. (Contributor), Colau, D. (Contributor), Ferain, T. (Contributor), Fraser, G. (Contributor), Galeni, M. (Contributor), Frere, J.-M. (Contributor), Masereel, B. (Contributor), Benoit, V. D. E. (Contributor), Wouters, J. (Contributor) & Frederick, R. (Contributor), Cambridge Crystallographic Data Centre, 1 Jan 2011
DOI: 10.5517/ccvnpfl, http://www.ccdc.cam.ac.uk/services/structure_request?id=doi:10.5517/ccvnpfl&sid=DataCite
Dataset