Simple di-and trivanillates exhibit cytostatic properties toward cancer cells resistant to pro-apoptotic stimuli

D Lamoral-Theys, L Pottier, F Kerff, F Dufrasne…

Index: Lamoral-Theys, Delphine; Pottier, Laurent; Kerff, Frederic; Dufrasne, Francois; Proutiere, Fabien; Wauthoz, Nathalie; Neven, Philippe; Ingrassia, Laurent; Antwerpen, Pierre Van; Lefranc, Florence; Gelbcke, Michel; Pirotte, Bernard; Kraus, Jean-Louis; Neve, Jean; Kornienko, Alexander; Kiss, Robert; Dubois, Jacques Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 11 p. 3823 - 3833

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Citation Number: 31

Abstract

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 IC50 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 ...