Synthesis of deoxyelephantopin analogues

J Antibiot (Tokyo). 2018 Feb;71(2):248-256. doi: 10.1038/ja.2017.132. Epub 2017 Nov 1.

Abstract

Deoxyelephantopin is a sesquiterpene lactone that was reported to be as effective in the treatment of mammary tumours and lung metastasis as taxol based on a murine orthotopic cancer model. Its germacrene skeleton harbours three Michael acceptors that can potentially engage a target covalently. Its strained 10-membered ring is densely functionalised and represents an important synthetic challenge. We herein describe our studies towards deoxyelephantopins using a ring-closing metathesis approach and report some unexpected observations.

MeSH terms

  • Antibiotics, Antineoplastic / chemical synthesis*
  • Indicators and Reagents
  • Lactones / chemical synthesis*
  • Molecular Conformation
  • Sesquiterpenes / chemical synthesis*

Substances

  • Antibiotics, Antineoplastic
  • Indicators and Reagents
  • Lactones
  • Sesquiterpenes
  • deoxyelephantopin