Antineoplastic Agents. 465. Structural Modification of Resveratrol: Sodium Resverastatin Phosphate
Journal of Medicinal Chemistry2002Vol. 45(12), pp. 2534–2542
Citations Over TimeTop 10% of 2002 papers
George R. Pettit, Matthew P. Grealish, M. Katherine Jung, Ernest Hamel, Robin K. Pettit, J.-Charles Chapuis, Jean M. Schmidt
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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