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- W3094901675 abstract "The synthesis and biological evaluation of truncated spirastrellolide A analogues comprised of the southern hemisphere against protein phosphatase 2A are described. A convergent synthesis was designed featuring two gold-catalyzed cyclization reactions, specifically, a dehydrative cyclization of monoallylic diols for the synthesis of the tetrahydropyran (A-ring) and a regioselective spiroketalization for the efficient generation of the [6,6]-spiroketal (B, C-ring system). The synthesis of the southern hemisphere of spirastrellolide A was achieved involving the longest linear sequence of 19 steps. A total of eight spirastrellolide A analogues were synthesized, and preliminary PP2A enzyme assay inhibition studies were performed for the first time on analogues of the southern hemisphere. Several analogues showed inhibition, which is a positive indication and perhaps suggests that the unsaturated spiroketal fragment might be crucial to induce PP2A inhibition." @default.
- W3094901675 created "2020-11-09" @default.
- W3094901675 creator A5052486739 @default.
- W3094901675 creator A5054475643 @default.
- W3094901675 creator A5071125447 @default.
- W3094901675 date "2020-10-28" @default.
- W3094901675 modified "2023-10-16" @default.
- W3094901675 title "Synthesis and Biological Evaluation of the Southern Hemisphere of Spirastrellolide A and Analogues" @default.
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- W3094901675 doi "https://doi.org/10.1021/acs.joc.0c01867" @default.
- W3094901675 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/33111529" @default.
- W3094901675 hasPublicationYear "2020" @default.
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