Insights into the structure–activity relationship of the anticancer compound ZJ-101, a derivative of marine natural product superstolide A: A role played by the lactone moiety

Haibo Qiu, Shan Qian, Sarah A. Head, Jun O. Liu, Zhendong Jin

Research output: Contribution to journalArticle

Abstract

Compound ZJ-101, a structurally simplified analog of the marine natural product superstolide A, was previously developed in our laboratory. In the subsequent structure–activity relationship study, a new analog ZJ-109 was designed and synthesized to probe the importance of the lactone moiety of the molecule by replacing the lactone in ZJ-101 with a lactam. The biological evaluation showed that ZJ-109 is about 8–12 times less active against cancer cells in vitro than ZJ-101, suggesting that the lactone moiety of the molecule is important for its anticancer activity.

Original languageEnglish (US)
Pages (from-to)4702-4704
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume26
Issue number19
DOIs
StatePublished - 2016

Keywords

  • Anticancer agent
  • Asymmetric synthesis
  • Drug design
  • Structure–activity relationship
  • Superstolide A analog

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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