Synthesis and biological activity of macrocyclic taxane analogues

Bioorg Med Chem Lett. 2004 May 17;14(10):2555-8. doi: 10.1016/j.bmcl.2004.02.086.

Abstract

A series of paclitaxel analogues possessing a macrocyclic structure between the 7 and 10 positions has been prepared. These compounds possess in vitro activity against a paclitaxel resistant cell line and have in vivo activity comparable to paclitaxel.

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Drug Resistance, Neoplasm
  • Humans
  • Inhibitory Concentration 50
  • Lung Neoplasms / drug therapy
  • Macrocyclic Compounds / chemical synthesis
  • Macrocyclic Compounds / pharmacology
  • Macrocyclic Compounds / therapeutic use
  • Mice
  • Neoplasms, Experimental / drug therapy
  • Paclitaxel / analogs & derivatives*
  • Structure-Activity Relationship
  • Taxoids / chemical synthesis*
  • Taxoids / pharmacology*
  • Taxoids / therapeutic use
  • Tubulin Modulators

Substances

  • Antineoplastic Agents
  • Macrocyclic Compounds
  • Taxoids
  • Tubulin Modulators
  • Paclitaxel