Design and 22-step synthesis of highly potent D-ring modified and linker-equipped analogs of spongistatin 1

Linda M. Suen; Makeda A. Tekle-Smith; Kevin S. Williamson; Joshua R. Infantine; Samuel K. Reznik; Paul S. Tanis; Tyler D. Casselman; Dan L. Sackett; James L. Leighton

doi:10.1038/s41467-018-07259-x

Nature Communications (Nov 2018)

Design and 22-step synthesis of highly potent D-ring modified and linker-equipped analogs of spongistatin 1

Linda M. Suen,
Makeda A. Tekle-Smith,
Kevin S. Williamson,
Joshua R. Infantine,
Samuel K. Reznik,
Paul S. Tanis,
Tyler D. Casselman,
Dan L. Sackett,
James L. Leighton

Affiliations

Linda M. Suen: Department of Chemistry, Columbia University
Makeda A. Tekle-Smith: Department of Chemistry, Columbia University
Kevin S. Williamson: Department of Chemistry, Columbia University
Joshua R. Infantine: Department of Chemistry, Columbia University
Samuel K. Reznik: Department of Chemistry, Columbia University
Paul S. Tanis: Department of Chemistry, Columbia University
Tyler D. Casselman: Department of Chemistry, Columbia University
Dan L. Sackett: Eunice Kennedy Shriver National Institute of Child Health and Human Development, National Institutes of Health
James L. Leighton: Department of Chemistry, Columbia University

DOI: https://doi.org/10.1038/s41467-018-07259-x
Journal volume & issue: Vol. 9, no. 1
pp. 1 – 8

Abstract

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Step-economical and efficient syntheses of Spongistatin 1 analogs are desirable for the development of potent anti-proliferative agents. Here, the authors report a 22-step synthesis of a D-ring modified Spongistatin 1 analog with retained picomolar potency among a group of C(15) ester derivatives.

Published in Nature Communications

ISSN: 2041-1723 (Online)
Publisher: Nature Portfolio
Country of publisher: United Kingdom
LCC subjects: Science
Website: https://www.nature.com/ncomms/

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