Antineoplastic agents. 592. Highly effective cancer cell growth inhibitory structural modifications of dolastatin 10

George Pettit, Fiona Hogan, Steven Toms

Research output: Contribution to journalArticle

29 Scopus citations


The dolastatin series of unique peptides, origi-nally discovered as constituents of the sea hare Dolabella auricularia, is of increasing importance in providing biological leads, especially to new and useful anticancer drugs. Dolastatin 10 and three analogues, minor structural modifications designated auristatins, are currently in human cancer clinical trials. The present study was undertaken to explore delivery to the cancer sites by way of phosphate or quinoline modifications. The initial objectives, auristatin TP as sodium phosphate 3b (GI50 10-2-10-4 μg/mL), auristatin 2-AQ (4, GI50 10-2-10-3 μg/mL), and auristatin 6-AQ (5, GI50 10-4 μg/mL), exhibited superior cancer cell growth inhibitory properties. (Chemical Equation Presented).

Original languageEnglish (US)
Pages (from-to)962-968
Number of pages7
JournalJournal of Natural Products
Issue number5
StatePublished - May 27 2011


ASJC Scopus subject areas

  • Analytical Chemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Complementary and alternative medicine
  • Organic Chemistry

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