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Synthesis and biological evaluation of a new class of bryostatin analogues: the role of the C20 substituent in protein kinase C binding

โœ Scribed by Paul A Wender; Kevin W Hinkle

Book ID
104210700
Publisher
Elsevier Science
Year
2000
Tongue
French
Weight
178 KB
Volume
41
Category
Article
ISSN
0040-4039

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โœฆ Synopsis

The synthesis and biological assay of a new series of designed bryostatin analogues modiยฎed at the C20 position are described. These compounds are found to bind to protein kinase C with anities of up to 1.5 nM, demonstrating that variations at C20 can indeed be used to tune anity and potentially function.

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## Abstract Herein, we report the synthesis of novel ringโ€expanded bryostatin analogues. By carefully modifying the substrate, a selective and highโ€yielding Ruโ€catalyzed tandem enyne coupling/Michael addition was employed to construct the northern fragment. Ringโ€closing metathesis was utilized to f