Total synthesis and initial biological evaluation of new B-ring-modified bryostatin analogs

Org Lett. 2006 Nov 9;8(23):5299-302. doi: 10.1021/ol0620904.

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.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Bryostatins
  • Macrolides / chemistry*
  • Macrolides / pharmacology*
  • Molecular Structure
  • Protein Binding
  • Protein Kinase C / chemistry
  • Protein Kinase C / metabolism

Substances

  • Antineoplastic Agents
  • Bryostatins
  • Macrolides
  • bryostatin 1
  • Protein Kinase C