ArticleJournal of the American Chemical Society2015
A "methyl extension" strategy for polyketide natural product linker site validation and its application to dictyostatin.
Article in Journal of the American Chemical Society, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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Who cites it
5 citing papers in PubMed, 13 citations in OpenAlex.
- Design and 22-step synthesis of highly potent D-ring modified and linker-equipped analogs of spongistatin 1.Nature communications · 2018Article
- Direct, Mild, and General n-BuOrganic letters · 2017Article
- Synthesis and Evaluation of a Linkable Functional Group-Equipped Analogue of the Epothilones.ACS medicinal chemistry letters · 2017Article
- Importance of a 4-Alkyl Substituent for Activity in the Englerin Series.ACS medicinal chemistry letters · 2017Article
- Article
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Authors and funding
3 authors at 2 institutions in 1 country.
Funding
Abstract
An approach to the validation of linker strategies for polyketide natural products with few or no obvious handles for linker attachment, and its application to dictyostatin, are described. Analogues in which the C(6)- and C(12)-methyl groups were replaced by 4-azidobutyl groups were prepared and shown to retain the low nanomolar potency of dictyostatin. Further, conjugation of the C(6) analogue with a cyclooctyne resulted in only minor attenuations in potency. Together, these results shed light on the binding of dictyostatin to β-tubulin, establish a validated linker strategy for dictyostatin, and set the stage for the synthesis and study of dictyostatin conjugates.
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