Role of the A-Ring of Bryostatin Analogues in PKC Binding:  Synthesis and Initial Biological Evaluation of New A-Ring-Modified Bryologs

The syntheses of three newly designed bryostatin analogues are reported. These simplified analogues, which lack the A-ring present in the natural product but possess differing groups at C9, were obtained using a divergent approach from a common intermediate. All three analogues exhibit potent, singl...

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Bibliographic Details
Published in:Organic letters 2005-05, Vol.7 (10), p.1995-1998
Main Authors: Wender, Paul A, Clarke, Michael O, Horan, Joshua C
Format: Article
Language:English
Subjects:
Animals
Binding Sites
Brain - enzymology
Bryostatins
Macrolides - chemical synthesis
Macrolides - chemistry
Macrolides - pharmacology
Molecular Structure
Protein Kinase C - chemistry
Protein Kinase C - metabolism
Rats
Structure-Activity Relationship
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Summary:The syntheses of three newly designed bryostatin analogues are reported. These simplified analogues, which lack the A-ring present in the natural product but possess differing groups at C9, were obtained using a divergent approach from a common intermediate. All three analogues exhibit potent, single-digit nanomolar affinity to protein kinase C.
ISSN:1523-7060
1523-7052
DOI:10.1021/ol0504650