2. Academic Validation
  3. Acetylated analogues of the microtubule-stabilizing agent discodermolide: preparation and biological activity

Acetylated analogues of the microtubule-stabilizing agent discodermolide: preparation and biological activity

  • J Nat Prod. 2001 Feb;64(2):171-4. doi: 10.1021/np000423e.
S P Gunasekera 1,  R E Longley,  R A Isbrucker
Affiliations

Affiliation

  • 1 Division of Biomedical Marine Research, Harbor Branch Oceanographic Institution, 5600 U.S. 1 North, Fort Pierce, Florida 34946, USA. [email protected]
PMID: 11429994 DOI: 10.1021/np000423e
Abstract

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.

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