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  • Title: Antineoplastic agents 337. Synthesis of dolastatin 10 structural modifications.
    Author: Pettit GR, Srirangam JK, Barkoczy J, Williams MD, Durkin KP, Boyd MR, Bai R, Hamel E, Schmidt JM, Chapuis JC.
    Journal: Anticancer Drug Des; 1995 Oct; 10(7):529-44. PubMed ID: 7495477.
    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.
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