Development of an advanced synthetic route to macrosphelides and its application to the discovery of a more potent macrosphelide derivative

Molecules. 2014 Sep 29;19(10):15572-83. doi: 10.3390/molecules191015572.

Abstract

The discovery of a more cytotoxic macrosphelide derivative, including its total synthesis and bioassay are described. Application of the Koide protocol to a readily available propagylic alcohol allowed the rapid and practical synthesis of a macrosphelide A skeleton. This strategy enabled the successful improvement of the cytotoxic activity of the macrosphelide derivative.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / toxicity
  • Biological Products / chemistry
  • Cell Line
  • Cell Survival / drug effects
  • Chemistry Techniques, Synthetic
  • Drug Discovery*
  • Heterocyclic Compounds / chemical synthesis
  • Heterocyclic Compounds / chemistry*
  • Heterocyclic Compounds / toxicity
  • Humans
  • Molecular Structure

Substances

  • Antineoplastic Agents
  • Biological Products
  • Heterocyclic Compounds