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  • Title: Vanillin-derived antiproliferative compounds influence Plk1 activity.
    Author: Carrasco-Gomez R, Keppner-Witter S, Hieke M, Lange L, Schneider G, Schubert-Zsilavecz M, Proschak E, Spänkuch B.
    Journal: Bioorg Med Chem Lett; 2014 Nov 01; 24(21):5063-9. PubMed ID: 25304894.
    Abstract:
    We synthesized a series of vanillin-derived compounds and analyzed them in HeLa cells for their effects on the proliferation of cancer cells. The molecules are derivatives of the lead compound SBE13, a potent inhibitor of the inactive conformation of human polo-like kinase 1 (Plk1). Some of the new designs were able to inhibit cancer cell proliferation to a similar extent as the lead structure. Two of the compounds ((({4-[(6-chloropyridin-3-yl)methoxy]-3-methoxyphenyl}methyl)(pyridin-4-ylmethyl)amine) and (({4-[(4-chlorophenyl)methoxy]-3-methoxyphenyl}methyl)(pyridin-4-ylmethyl)amine)) were much stronger in their capacity to reduce HeLa cell proliferation and turned out to potently induce apoptosis and reduce Plk1 kinase activity in vitro.
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