title: Lead Diversification through a Prins-Driven Macrocyclization Strategy: Application to C13-Diversified Bryostatin Analogues.
abstract: The design, synthesis, and biological evaluation of a novel class of C13-diversified bryostatin analogues are described. An innovative and general strategy based on a Prins macrocyclization-nucleophilic trapping cascade was used to achieve late-stage diversification. In vitro analysis of selected library members revealed that modification at the C13 position of the bryostatin scaffold can be used as a diversification handle to regulate biological activity.
authors.affiliation: Department of Chemistry, Department of Chemical and Systems Biology, Stanford University, Stanford, CA 94305-5080, USA, Fax +1(650)7250259.
authors.forename: Paul A
authors.initials: PA
authors.lastname: Wender
authors.affiliation: Department of Radiology, Stanford University School of Medicine, Stanford, CA 94305-5105, USA.
authors.forename: Kelvin L
authors.initials: KL
authors.lastname: Billingsley
keywords: cyclizations; drugs; macrocycles; polyketides