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

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.

SUBMITTER: Lamoral-Theys D

PROVIDER: S-EPMC4966668 | biostudies-literature | 2010 Jun

REPOSITORIES: biostudies-literature

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

Lamoral-Theys Delphine D Pottier Laurent L Kerff Frédéric F Dufrasne François F Proutière Fabien F Wauthoz Nathalie N Neven Philippe P Ingrassia Laurent L Antwerpen Pierre Van PV Lefranc Florence F Gelbcke Michel M Pirotte Bernard B Kraus Jean-Louis JL Nève Jean J Kornienko Alexander A Kiss Robert R Dubois Jacques J

Bioorganic & medicinal chemistry 20100421 11

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 de ...[more]

PMID: 20466556

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