Keywords :
Apoptosis/drug effects; Cell Cycle Proteins/antagonists & inhibitors; Cytostatic Agents/chemical synthesis/pharmacology; Inhibitory Concentration 50; Neoplasms/drug therapy/pathology; Nuclear Proteins/antagonists & inhibitors; Protein-Serine-Threonine Kinases/antagonists & inhibitors; Protein-Tyrosine Kinases/antagonists & inhibitors; Structure-Activity Relationship; Vanillic Acid/chemical synthesis/pharmacology/therapeutic use
Abstract :
[en] 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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