Antineoplastic agents. 465. Structural modification of resveratrol: Sodium resverastatin phosphate

George Pettit, Matthew P. Grealish, M. Katherine Jung, Ernest Hamel, Robin Pettit, Jean Chapuis, Jean M. Schmidt

Research output: Contribution to journalArticle

156 Scopus citations

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 (GI50 = 0.01-0.001 μg/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.

Original languageEnglish (US)
Pages (from-to)2534-2542
Number of pages9
JournalJournal of Medicinal Chemistry
Volume45
Issue number12
DOIs
StatePublished - Jun 6 2002

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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