Facile Synthetic Access to and Biological Evaluation of the Macrocyclic Core of Apoptolidin

Oxidative cleavage of the C-20/C-21 bond in apoptolidin (1) provides two fragments of similar complexity, facilitating a divide-and-diversify strategy for the determination of the structural basis for apoptolidin's biological activity, the remarkably selective induction of apoptosis in sensitiv...

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Bibliographic Details
Published in:Organic letters 2003-06, Vol.5 (13), p.2299-2302
Main Authors: Wender, Paul A, Jankowski, Orion D, Tabet, Elie A, Seto, Haruo
Format: Article
Language:English
Subjects:
Apoptosis - drug effects
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Inhibitory Concentration 50
Macrolides - chemistry
Macrolides - pharmacology
Methanol - chemistry
Mitochondrial Proton-Translocating ATPases - antagonists & inhibitors
Oxidation-Reduction
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Summary:Oxidative cleavage of the C-20/C-21 bond in apoptolidin (1) provides two fragments of similar complexity, facilitating a divide-and-diversify strategy for the determination of the structural basis for apoptolidin's biological activity, the remarkably selective induction of apoptosis in sensitive cell lines. The ability of compounds derived from this cleavage to inhibit mitochondrial F0F1-ATPase is reported.
ISSN:1523-7060
1523-7052
DOI:10.1021/ol0346335