Bioactive diterpenoid containing a reversible "spring-loaded" (E,Z)-dieneone Michael acceptor

Org Lett. 2011 Aug 5;13(15):3920-3. doi: 10.1021/ol201443k. Epub 2011 Jul 12.

Abstract

Three new briarane diterpenoids, briareolate esters L-N (1-3), have been isolated from a gorgonian Briareum asbestinum. Briareolate esters L (1) and M (2) are the first natural products possessing a 10-membered macrocyclic ring with a (E,Z)-dieneone and exhibit growth inhibition activity against both human embryonic stem cells (BG02) and a pancreatic cancer cell line (BxPC-3). Briareolate ester L (1) was found to contain a "spring-loaded" (E,Z)-dieneone Michael acceptor group that can form a reversible covalent bond to model sulfur-based nucleophiles.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Anthozoa / chemistry*
  • Biological Products / chemistry
  • Biological Products / isolation & purification
  • Cell Line
  • Diterpenes / chemistry*
  • Diterpenes / isolation & purification
  • Humans
  • Models, Molecular
  • Molecular Structure

Substances

  • Biological Products
  • Diterpenes