Journal
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
Volume 130, Issue 21, Pages 6658-+Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ja8015632
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Funding
- NCI NIH HHS [CA31845, R37 CA031845-28, R37 CA031845, R01 CA031845] Funding Source: Medline
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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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