Abstract
A ring expanded bryostatin analogue was synthesized by utilizing a Ru-catalyzed tandem tetrahydropyran formation, a Pd-catalyzed tandem dihydropyran formation, and a ring-closing metathesis (RCM) as key steps. The analogue possesses potent anti-tumor activity against the NCI-ADR cancer cell line with an IC50 of 123 nM.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Drug Screening Assays, Antitumor
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Humans
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Macrolides / chemical synthesis*
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Macrolides / chemistry
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Macrolides / pharmacology
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Molecular Conformation
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Stereoisomerism
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Structure-Activity Relationship