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, single-digit nanomolar affinity to protein kinase C.