Synthesis and evaluation of double bond substituted combretastatins

Eur J Med Chem. 2005 Jun;40(6):529-41. doi: 10.1016/j.ejmech.2004.12.008.

Abstract

A series of combretastatins substituted with epoxides, amides and small alkyl groups has been synthesised and evaluated for cytotoxicity and their ability to inhibit the assembly of tubulin. The methyl and ethyl substituted phenols 36, 44 have shown potent antimitotic effects whilst exhibiting reduced cytotoxicity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemical synthesis
  • Amides / chemistry
  • Amides / pharmacology
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Bibenzyls / chemical synthesis*
  • Bibenzyls / chemistry
  • Bibenzyls / pharmacology*
  • Cell Cycle / drug effects
  • Cell Survival / drug effects
  • Epoxy Compounds / chemical synthesis
  • Epoxy Compounds / chemistry
  • Epoxy Compounds / pharmacology
  • Formazans / chemistry
  • Humans
  • Inhibitory Concentration 50
  • K562 Cells
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Spectrophotometry, Ultraviolet
  • Stilbenes / chemical synthesis*
  • Stilbenes / chemistry
  • Stilbenes / pharmacology*
  • Tetrazolium Salts / chemistry
  • Tubulin / metabolism
  • Tubulin Modulators

Substances

  • Amides
  • Antineoplastic Agents
  • Bibenzyls
  • Epoxy Compounds
  • Formazans
  • Stilbenes
  • Tetrazolium Salts
  • Tubulin
  • Tubulin Modulators
  • MTT formazan
  • combretastatin