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Antineoplastic agents 337. Synthesis of dolastatin 10 structural modifications
G R Pettit1, J K Srirangam, J Barkoczy
1Cancer Research Institute, Arizona State University, Tempe 85287-16-4, USA.
Anti-Cancer Drug Design
|October 1, 1995
Abstract:
New structural modifications of the marine shell-less mollusk peptide constituent dolastatin 10 (1) have been synthesized, and evaluated against a variety of cancer cell lines and for their ability to inhibit tubulin polymerization. A number of useful structure-activity relationships were uncovered. The most important observation was that the dolaphenine unit of dolastatin 10 could be satisfactorily replaced with a phenethylamine. Peptide 11C, designated auristatin PE, was found to exhibit inhibition of cancer cell growth and tubulin assembly comparable to that of dolastatin 10.