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Bioorg Med Chem. 2010 Jun 1;18(11):3823-33. doi: 10.1016/j.bmc.2010.04.047. Epub 2010 Apr 21.

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

Author information

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

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.

PMID:
20466556
PMCID:
PMC4966668
DOI:
10.1016/j.bmc.2010.04.047
[Indexed for MEDLINE]
Free PMC Article
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