Synthesis and antitumor activity of epothilone B

Eur J Med Chem. 2018 Sep 5:157:925-934. doi: 10.1016/j.ejmech.2018.08.055. Epub 2018 Aug 23.

Abstract

Epothilones are a class of 16-membered macrolide compounds targeting microtubules. They have good anticancer activity and their mechanism of action is similar to that of paclitaxel. Epothilones are also highly active against cancer cells that are resistant to paclitaxel and other anticancer drugs. They have good water solubility, simple structure, and are relatively easy to totally synthesize and or semi-synthesize. These results immediately attracted great interest and research enthusiasm from pharmaceutical companies and academia. Herein, the various synthetic methods of epothilone B and its anticancer activity were summarized and analyzed.

Keywords: Antitumor activity; Epothilone B; Semi-synthesize; Targeting microtubules; Totally synthesize.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Epothilones / chemical synthesis*
  • Epothilones / chemistry
  • Epothilones / pharmacology*
  • Humans
  • Molecular Structure
  • Neoplasms / drug therapy*
  • Neoplasms / pathology
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Epothilones
  • epothilone B