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Design, synthesis, and biological evaluation of a potent, PKC selective, B-ring analog of bryostatin
Paul A Wender1, Vishal A Verma
1Department of Chemistry, Stanford University, Stanford, California 94305-5080, USA. wenderp@stanford.edu
Abstract:
[structure: see text] The first member of a new class of five-membered B-ring analogs of bryostatin has been synthesized and tested for its ability to bind and translocate protein kinase C (PKC). This synthesis extends the utility of our previously introduced macrotransacetalization strategy to the formation of five-membered dioxolane B-ring analogs. This analog exhibits potent, single-digit nanomolar affinity to PKC and selectively translocates novel PKC isozymes.
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