Bioorganic & Medicinal Chemistry 2010-06-01

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

Delphine Lamoral-Theys, 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

Index: Bioorg. Med. Chem. 18 , 3823-33, (2010)

Full Text: HTML

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.

Related Compounds

  • Vanillic acid
  • Methyl vanillate

Related Articles:

Antimicrobial activity of natural products from the flora of Northern Ontario, Canada.

2015-06-01

[Pharm. Biol. 53(6) , 800-6, (2015)]

Comparison between ATR-IR, Raman, concatenated ATR-IR and Raman spectroscopy for the determination of total antioxidant capacity and total phenolic content of Chinese rice wine.

2016-03-01

[Food Chem. 194 , 671-9, (2015)]

Antagonistic control of a dual-input mammalian gene switch by food additives.

2014-08-01

[Nucleic Acids Res. 42(14) , e116, (2014)]

Synthesis and accumulation of aromatic aldehydes in an engineered strain of Escherichia coli.

2014-08-20

[J. Am. Chem. Soc. 136(33) , 11644-54, (2014)]

Optimization of antioxidant phenolic compounds extraction from quinoa (Chenopodium quinoa) seeds.

2015-07-01

[J. Food Sci. Technol. 52 , 4396-404, (2015)]

More Articles...