New sources of chemical diversity inspired by biosynthesis: rational design of a potent epothilone analogue

Org Lett. 2009 Aug 6;11(15):3186-9. doi: 10.1021/ol900971r.

Abstract

A concise total synthesis of (S)-14-methoxyepothilone D has been accomplished. (S)-14-Methoxyepothilone D represents a conceptually novel example of polyketide analogue design based on an alternative biogenetic pattern of extender units. The significant biological activity observed for this compound provides a foundation to support studies designed to prepare derivatives of this type through fermentation of genetically engineered organisms expressing the epothilone PKS gene cluster.

Publication types

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

MeSH terms

  • Cell Line, Tumor
  • Epothilones / chemical synthesis*
  • Epothilones / chemistry
  • Epothilones / pharmacology
  • Humans
  • Macrolides / chemical synthesis
  • Macrolides / chemistry*
  • Macrolides / pharmacology
  • Structure-Activity Relationship

Substances

  • (S)-14-methoxyepothilone
  • Epothilones
  • Macrolides
  • epothilone C
  • desoxyepothilone B