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  • Title: Antineoplastic agents. 465. Structural modification of resveratrol: sodium resverastatin phosphate.
    Author: Pettit GR, Grealish MP, Jung MK, Hamel E, Pettit RK, Chapuis JC, Schmidt JM.
    Journal: J Med Chem; 2002 Jun 06; 45(12):2534-42. PubMed ID: 12036362.
    Abstract:
    As an extension of structure/activity investigations of resveratrol (1), phenstatin (2c), and the cancer antiangiogenesis drug sodium combretastatin A-4 phosphate (2b), syntheses of certain related stilbenes (14) and benzophenones (16) were undertaken. The trimethyl ether derivative of (Z)-resveratrol (4a) exhibited the strongest activity (GI(50) = 0.01-0.001 microg/mL) against a minipanel of human cancer cell lines. A monodemethylated derivative (14c) was converted to prodrug 14n (sodium resverastatin phosphate) for further biological evaluation. The antitubulin and antimicrobial activities of selected compounds were also evaluated.
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