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

Bioorg Med Chem. 2010 Jun 1;18(11):3823-33. doi: 10.1016/j.bmc.2010.04.047.

Delphine Lamoral-Theys ¹, Laurent Pottier, Frédéric Kerff, François Dufrasne, Fabien Proutière, Nathalie Wauthoz, Philippe Neven, Laurent Ingrassia, Pierre Van Antwerpen, Florence Lefranc, Michel Gelbcke, Bernard Pirotte, Jean-Louis Kraus, Jean Nève, Alexander Kornienko, Robert Kiss, Jacques Dubois

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Affiliation

1 Institut de Pharmacie, Université Libre de Bruxelles, Brussels, Belgium.

PMID: 20466556 DOI: 10.1016/j.bmc.2010.04.047

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 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.

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