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

George Pettit; Fiona Hogan; Steven Toms

doi:10.1021/np1007334

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

George Pettit, Fiona Hogan, Steven Toms

Research output: Contribution to journal › Article › peer-review

42 Scopus citations

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 language	English (US)
Pages (from-to)	962-968
Number of pages	7
Journal	Journal of Natural Products
Volume	74
Issue number	5
DOIs	https://doi.org/10.1021/np1007334
State	Published - 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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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).",

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

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