Org. Lett., 8 (20), 4581 -4584, 2006. 10.1021/ol0618149 S1523-7060(06)01814-1
Web Release Date: September 2, 2006

Copyright © 2006 American Chemical Society

Synthesis and PKC Binding of a New Class of A-Ring Diversifiable Bryostatin Analogues Utilizing a Double Asymmetric Hydrogenation and Cross-Coupling Strategy

Paul A. Wender* and Joshua C. Horan

Department of Chemistry, Stanford University, Stanford, California 94305-5080, and Department of Molecular Pharmacology, Stanford University School of Medicine, Stanford University, Stanford, California 94305-5080

wenderp@stanford.edu

Received July 23, 2006

Abstract:

The design, asymmetric synthesis, and biological evaluation of a new class of bryostatin analogues based on a pseudosymmetric spacer domain are described. An aryl bromide diversification site is incorporated allowing access to systematically varied analogues. The new analogues all exhibit potent, nanomolar affinity to PKC.


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