Reference : Simple di- and trivanillates exhibit cytostatic properties toward cancer cells resist...
Scientific journals : Article
Human health sciences : Oncology
http://hdl.handle.net/2268/74927
Simple di- and trivanillates exhibit cytostatic properties toward cancer cells resistant to pro-apoptotic stimuli.
English
Lamoral-Theys, Delphine [> > > >]
Pottier, Laurent [> > > >]
Kerff, Frédéric mailto [Université de Liège - ULg > > Centre d'ingénierie des protéines >]
Dufrasne, Francois [> > > >]
Proutiere, Fabien [> > > >]
Wauthoz, Nathalie [> > > >]
Neven, Philippe [> > > >]
Ingrassia, Laurent [> > > >]
Antwerpen, Pierre Van [> > > >]
Lefranc, Florence [> > > >]
Gelbcke, Michel [> > > >]
Pirotte, Bernard mailto [Université de Liège - ULg > Département de pharmacie > Chimie pharmaceutique >]
Kraus, Jean*-Louis [> > > >]
Neve, Jean [> > > >]
Kornienko, Alexander [> > > >]
Kiss, Robert [> > > >]
Dubois, Jacques [Université de Liège - ULg > Services généraux (Faculté de philosophie et lettres) > Relations académiques et scientifiques (Philo et lettres) >]
2010
Bioorganic & Medicinal Chemistry
Elsevier Science
18
11
3823-33
Yes (verified by ORBi)
International
0968-0896
1464-3391
Oxford
United Kingdom
[en] Apoptosis/drug effects ; Cell Cycle Proteins/antagonists & inhibitors ; Cytostatic Agents/chemical synthesis/pharmacology ; Inhibitory Concentration 50 ; Neoplasms/drug therapy/pathology ; Nuclear Proteins/antagonists & inhibitors ; Protein-Serine-Threonine Kinases/antagonists & inhibitors ; Protein-Tyrosine Kinases/antagonists & inhibitors ; Structure-Activity Relationship ; Vanillic Acid/chemical synthesis/pharmacology/therapeutic use
[en] A series of 33 novel divanillates and trivanillates were synthesized and found to possess promising cytostatic rather than cytotoxic properties. Several compounds under study decreased by >50% the activity of Aurora A, B, and C, and WEE1 kinase activity at concentrations <10% of their IC(50) growth inhibitory ones, accounting, at least partly, for their cytostatic effects in cancer cells and to a lesser extent in normal cells. Compounds 6b and 13c represent interesting starting points for the development of cytostatic agents to combat cancers, which are naturally resistant to pro-apoptotic stimuli, including metastatic malignancies.
Centre d'Ingénierie des Protéines - CIP
http://hdl.handle.net/2268/74927
10.1016/j.bmc.2010.04.047

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