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
Affiliations
  • 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.