Acetylated analogues of the microtubule-stabilizing agent discodermolide: preparation and biological activity.
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.
Gunasekera
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SP
Division of Biomedical Marine Research, Harbor Branch Oceanographic Institution, 5600 U.S. 1 North, Fort Pierce, Florida 34946, USA. sgunaseker@hboi.edu
Longley
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Isbrucker
R A
RA
D000107:Acetylation; D000473:Alkanes; D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D002219:Carbamates; D007783:Lactones / Q000737:chemistry* / Q000494:pharmacology; D007941:Leukemia P388 / Q000188:drug therapy; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D008870:Microtubules / Q000187:drug effects*; D008956:Models, Chemical; D011161:Porifera / Q000737:chemistry; D011753:Pyrones
D000473:Alkanes; D000970:Antineoplastic Agents; D002219:Carbamates; D007783:Lactones; D011753:Pyrones; C071229:discodermolide