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Updated: Jul 19, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Total synthesis and initial biological evaluation of new B-ring-modified bryostatin analogs
Paul A Wender1, Joshua C Horan, Vishal A Verma
1Department of Chemistry, Stanford University, Stanford, California 94305-5080, USA. wenderp@stanford.edu
Abstract:
[Structure: see text] The total synthesis and preliminary biological evaluation of the first bryostatin analogs (bryologs) to incorporate B-ring substitution are reported. Asymmetric syntheses of two new polyketide "spacer" domains are described, one exploiting the pseudosymmetry of the C1-C13 region. These fragments are convergently joined to the "recognition" domain through a remarkably versatile macrotransacetalization process. The resulting new analogs exhibit potent nanomolar or picomolar affinity to protein kinase C (PKC), comparable to or better than that found for bryostatin.
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