Indol-2-yl ethanones as novel indoleamine 2,3-dioxygenase (IDO) inhibitors.
; ; et al
in Bioorganic & Medicinal Chemistry (2011), 19(4), 1550-61
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 ... [more ▼]
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. [less ▲]Detailed reference viewed: 49 (6 ULg)
Bis-tetrahydroisoquinoline derivatives: Structure analysis of the three stereoisomers of 1,1'-(propane-1,3-diyl)-bis-(6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydroisoquinoline)
; ; et al
in European Journal of Medicinal Chemistry (2010), 45Detailed reference viewed: 25 (3 ULg)
Impact of the Crystallinity on the Physical Properties of Inulin during Water Sorption
; Paquot, Michel ; Blecker, Christophe et al
in Food Biophysics (2009), 4(1), 49-58
The impact of the crystallinity of spray-dried inulins on their stability and physical properties was investigated after a conditioning of 1 week at different relative humidity levels (0% to 94%) at 20 A ... [more ▼]
The impact of the crystallinity of spray-dried inulins on their stability and physical properties was investigated after a conditioning of 1 week at different relative humidity levels (0% to 94%) at 20 A degrees C. An environmental scanning electron microscopy study showed that the amorphous powders hardened at a relative humidity storage between 59% and 75%; while their semi-crystalline counterparts were partially agglomerated but friable in the same conditions. Caking was observed when the glass transition temperature of the amorphous phase of the material dropped below the storage temperature of the powder. It resulted in a crystallization of the structural units of varying lengths composing inulin, but also an increase of the crystallinity of the semi-crystalline ones. This study showed the importance of the crystallinity of inulin on its stability and physical properties during storage which is of crucial importance for the shelf-life of food and pharmaceutical products in the dry state. [less ▲]Detailed reference viewed: 29 (5 ULg)
Caking phenomena and physical parameters of amorphous inulin related to adsorption and desorption isotherms.
; Paquot, Michel ; et al
Poster (2006, March)Detailed reference viewed: 16 (1 ULg)
Characterization of inulin stored at different relative humidities by MDSC and X-ray diffraction, related to soption isotherms.
; ; Paquot, Michel et al
Poster (2004, December)Detailed reference viewed: 29 (15 ULg)