Efficient synthetic access to a new family of highly potent bryostatin analogues via a Prins-driven macrocyclization strategy |
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Authors: | Wender Paul A Dechristopher Brian A Schrier Adam J |
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Affiliation: | Departments of Chemistry and Chemical and Systems Biology, Stanford University, Stanford, California 94305-5080, USA. wenderp@stanford.edu |
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Abstract: | The step-economical synthesis of a new class of bryostatin analogues that contain the complete oxycarbocyclic core ring system of the bryostatin natural products is reported. These agents are convergently assembled via a highly efficient, functional-group-tolerant, and stereoselective Prins-driven macrocyclization. These tetrahydropyranyl B-ring analogues are among our most potent and efficacious analogues to date, exhibiting nanomolar and picomolar activities in protein kinase C affinity assays as well as in cellular antiproliferation assays. |
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