Synthesis and antiproliferativeactivity of new vinca alkaloids containing an α,β-unsaturated aromatic side chain

Bioorg Med Chem Lett. 2015 Dec 1;25(23):5597-600. doi: 10.1016/j.bmcl.2015.10.040. Epub 2015 Oct 23.

Abstract

A new series of vinca-alkaloids derivatives containing various α,β-unsaturated aromatic side chains was synthesized. Four new vinca-alkaloids derivatives showed selective cytotoxicities against KB tumor cell lines with IC50 value below 0.1 μM, thus comparable with vinblastine.

Keywords: Cytotoxicity; Sarcodictyins; Tubulin; Vinca alkaloids.

MeSH terms

  • Antineoplastic Agents, Phytogenic / chemical synthesis*
  • Antineoplastic Agents, Phytogenic / chemistry
  • Antineoplastic Agents, Phytogenic / therapeutic use*
  • Cell Line, Tumor
  • Humans
  • Inhibitory Concentration 50
  • Molecular Structure
  • Neoplasms / drug therapy*
  • Vinblastine / chemistry
  • Vinblastine / therapeutic use*
  • Vinca Alkaloids / chemistry

Substances

  • Antineoplastic Agents, Phytogenic
  • Vinca Alkaloids
  • Vinblastine