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

28 Citations (Scopus)

Abstract

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
Volume74
Issue number5
DOIs
StatePublished - May 27 2011

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dolastatin 10
Cell growth
Antineoplastic Agents
Growth
Neoplasms
Hares
Oceans and Seas
Phosphates
Clinical Trials
Peptides
auristatin
Pharmaceutical Preparations

ASJC Scopus subject areas

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

Cite this

Antineoplastic agents. 592. Highly effective cancer cell growth inhibitory structural modifications of dolastatin 10. / Pettit, George; Hogan, Fiona; Toms, Steven.

In: Journal of Natural Products, Vol. 74, No. 5, 27.05.2011, p. 962-968.

Research output: Contribution to journalArticle

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