Structure-activity relationships within a family of selectively cytotoxic macrolide natural products

Arthur R. Salomon, Yongbo Zhang, Haruo Seto, Chaitan Khosla*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

44 Scopus citations

Abstract

(equation presented) We describe a semi-synthetic deglycosylated derivative of apoptolidin that retains considerable activity against the mitochondrial ATPase but has greatly reduced cellular cytotoxicity. We also demonstrate that a related antifungal natural product, cytovaricin, inhibits the same molecular target. Structural comparison of these macrolides provides insights into their conserved features that are presumably important for biological activity and identifies promising avenues at the interface of organic synthesis and biosynthesis for the generation of new selective cytotoxic agents.

Original languageEnglish (US)
Pages (from-to)57-59
Number of pages3
JournalOrganic Letters
Volume3
Issue number1
DOIs
StatePublished - Jan 11 2001

ASJC Scopus subject areas

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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