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J Nat Prod. 2011 May 27;74(5):962-8. doi: 10.1021/np1007334. Epub 2011 May 2.

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

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1
Cancer Research Institute and Department of Chemistry and Biochemistry, Arizona State University, P.O. Box 871604, Tempe, Arizona 85287-1604, United States.

Abstract

The dolastatin series of unique peptides, originally 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.

PMID:
21534541
PMCID:
PMC3116808
DOI:
10.1021/np1007334
[Indexed for MEDLINE]
Free PMC Article
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