Diversity-Oriented Library Synthesis from Steviol and Isosteviol-Derived Scaffolds

Trinh A.D. Holth, Michael A. Walters, Oliver E. Hutt, Gunda I. Georg

Research output: Contribution to journalArticlepeer-review

Abstract

The readily available natural product stevioside provides a unique diterpene core structure that can be explored for small molecule library development by diversity-oriented synthesis and functional group transformations. Validation arrays were prepared from steviol, isosteviol, and related analogues, derived from stevioside, to produce over 90 compounds. These compounds were submitted to the NIH Molecular Libraries Small Molecule Repository for screening in the Molecular Libraries Screening Center Network. Micromolar hits were identified in multiple high-throughput assays for several library members. A cheminformatics analysis of the compounds was performed that verified the expected diversity and complexity of this set of compounds. The screening results indicate that scaffolds-derived natural products can provide screening hits against multiple target proteins.

Original languageEnglish (US)
Pages (from-to)150-155
Number of pages6
JournalACS Combinatorial Science
Volume22
Issue number3
DOIs
StatePublished - Mar 9 2020

Bibliographical note

Funding Information:
We gratefully acknowledge financial support from the National Institutes of Health (Grant GM081267) and the University of Minnesota through the Vince and McKnight Endowed Chairs.

Publisher Copyright:
Copyright © 2020 American Chemical Society.

Copyright:
Copyright 2020 Elsevier B.V., All rights reserved.

Keywords

  • DOS
  • analogues
  • isosteviol
  • library synthesis
  • steviol

PubMed: MeSH publication types

  • Journal Article
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

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