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  • Title: Semisynthetic analogues of the microtubule-stabilizing agent discodermolide: preparation and biological activity.
    Author: Gunasekera SP, Longley RE, Isbrucker RA.
    Journal: J Nat Prod; 2002 Dec; 65(12):1830-7. PubMed ID: 12502323.
    Abstract:
    A series of 12 semisynthetic discodermolide analogues, 2-13, have been prepared using natural (+)-discodermolide (1) and evaluated for in vitro cytotoxicity against cultured murine P-388 leukemia and A-549 human adenocarcinoma cells. These semisynthetic analogues showed a significant variation of cytotoxicity and confirmed the importance of the C-7 through C-19 molecular fragment for potency. Specifically, these analogues suggested the importance of the C-11 and C-17 hydroxyl groups and the C-13 double bond for the potency of discodermolide. The preparation, structure elucidation, and biological activity of these new analogues are described.
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