Projects per year
Abstract
Tsitsikammamines are marine alkaloids whose structure is based on the pyrroloiminoquinone scaffold. These and related compounds have attracted attention due to various interesting biological properties, including cytotoxicity, topoisomerase inhibition, antimicrobial, antifungal and antimalarial activity. Indoleamine 2,3-dioxygenase (IDO1) is a well-established therapeutic target as an important factor in the tumor immune evasion mechanism. In this preliminary communication, we report the inhibitory activity of tsitsikammamine derivatives against IDO1. Tsitsikammamine A analogue 11b displays submicromolar potency in an enzymatic assay. A number of derivatives are also active in a cellular assay while showing little or no activity towards tryptophan 2,3-dioxygenase (TDO), a functionally related enzyme. This IDO1 inhibitory activity is rationalized by molecular modeling studies. An interest is thus established in this class of compounds as a potential source of lead compounds for the development of new pharmaceutically useful IDO1 inhibitors.
Original language | English |
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Pages (from-to) | 47-54 |
Number of pages | 8 |
Journal | Bioorganic and medicinal chemistry letters |
Volume | 23 |
Issue number | 1 |
Early online date | 24 Nov 2012 |
DOIs | |
Publication status | Published - 1 Jan 2013 |
Event | JFB 2011. - Liege, Belgium Duration: 19 May 2011 → … |
Keywords
- Cancer immunology
- Indoleamine 2,3-dioxygenase
- Molecular modeling
- Pyrroloiminoquinones
- Tsitsikammamines
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Projects
- 1 Finished
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CANTOL: Design and synthesis of indolamine dioxygenase (IDO) for the treatment of cancer
MASEREEL, B., Wouters, J., Dolušić, E., FREDERICK, R., POUYEZ, J., Van den Eynde, B. J., Frère, J., Moser, M., Jean-Marie, B., Combalbert, J. & Stephenne, J.
1/04/08 → 31/03/12
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
- 5 Participation in conference
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47th RICT: Drug Discovery and Selection.
Eduard Dolusic (Poster)
6 Jul 2011 → 8 Jul 2011Activity: Participating in or organising an event types › Participation in conference
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JFB 2011.
Eduard Dolusic (Speaker)
19 May 2011 → 20 May 2011Activity: Participating in or organising an event types › Participation in conference
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XVIIIeme JOURNEE JEUNES CHERCHEURS
Eduard Dolusic (Poster)
4 Feb 2011Activity: Participating in or organising an event types › Participation in conference