- Simple di- and trivanillates exhibit cytostatic properties toward cancer cells resistant to pro-apoptotic stimuli
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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 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.
- Lamoral-Theys, Delphine,Pottier, Laurent,Kerff, Frédéric,Dufrasne, Fran?ois,Proutière, Fabien,Wauthoz, Nathalie,Neven, Philippe,Ingrassia, Laurent,Antwerpen, Pierre Van,Lefranc, Florence,Gelbcke, Michel,Pirotte, Bernard,Kraus, Jean-Louis,Nève, Jean,Kornienko, Alexander,Kiss, Robert,Dubois, Jacques
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experimental part
p. 3823 - 3833
(2010/08/19)
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- DI-VANILLOYL AND TRI-VANILLOYL DERIVATIVES FOR USE IN ANTI-CANCER THERAPY
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The invention relates to the medical field, more precisely in the field of anti-cancer treatment and treatment of Alzheimer's disease, Parkinson's disease or Pick's disease or for ameliorating symptoms of Down syndrome, providing newly synthesised multi-vanilloyl derivative compounds and their use in the treatment of said disorders.
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Page/Page column 47
(2010/04/30)
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