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Acetylated Analogues of the Microtubule-Stabilizing Agent Discodermolide: Preparation and Biological Activity

2001; American Chemical Society; Volume: 64; Issue: 2 Linguagem: Inglês

10.1021/np000423e

1520-6025

Sarath P. Gunasekera, Ross E. Longley, Richard Isbrucker,

Synthetic Organic Chemistry Methods

A series of eight discodermolide acetates have been prepared using natural (+)-discodermolide and evaluated for in vitro cytotoxicity against the cultured murine P-388 leukemia cells. The acetylated analogues showed a significant variation of cytotoxicity and suggested the importance of C-11 and C-17 hydroxyl groups for potency. The preparation and structure elucidation of the new analogues are described.