Article (Scientific journals)
Simple di- and trivanillates exhibit cytostatic properties toward cancer cells resistant to pro-apoptotic stimuli.
Lamoral-Theys, Delphine; Pottier, Laurent; Kerff, Frédéric et al.
2010In Bioorganic and Medicinal Chemistry, 18 (11), p. 3823-33
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Keywords :
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
Abstract :
[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.
Research center :
CIP - Centre d'Ingénierie des Protéines - ULiège
Disciplines :
Oncology
Author, co-author :
Lamoral-Theys, Delphine
Pottier, Laurent
Kerff, Frédéric  ;  Université de Liège - ULiège > Centre d'ingénierie des protéines
Dufrasne, Francois
Proutiere, Fabien
Wauthoz, Nathalie
Neven, Philippe
Ingrassia, Laurent
Antwerpen, Pierre Van
Lefranc, Florence
Gelbcke, Michel
Pirotte, Bernard ;  Université de Liège - ULiège > Département de pharmacie > Chimie pharmaceutique
Kraus, Jean*-Louis
Neve, Jean
Kornienko, Alexander
Kiss, Robert
Dubois, Jacques ;  Université de Liège - ULiège > Services généraux (Faculté de philosophie et lettres) > Relations académiques et scientifiques (Philo et lettres)
More authors (7 more) Less
Language :
English
Title :
Simple di- and trivanillates exhibit cytostatic properties toward cancer cells resistant to pro-apoptotic stimuli.
Publication date :
2010
Journal title :
Bioorganic and Medicinal Chemistry
ISSN :
0968-0896
eISSN :
1464-3391
Publisher :
Elsevier Science, Oxford, United Kingdom
Volume :
18
Issue :
11
Pages :
3823-33
Peer reviewed :
Peer Reviewed verified by ORBi
Available on ORBi :
since 03 November 2010

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