Antitumor activity of unsaturated fatty acid esters of 4'-demethyldeoxypodophyllotoxin

Bioorg Med Chem Lett. 2003 Aug 18;13(16):2629-32. doi: 10.1016/s0960-894x(03)00558-4.

Abstract

Unsaturated fatty acid esters of 4'-demethyldeoxypodophyllotoxin (DDPT) were prepared and tested for antitumor activity. The esters showed increased in vivo antitumor activity despite the lower in vitro activity than DDPT. Especially, the ester (DFE12) of all-cis-11,14-eicosadienoic acid was much better (IR, 83%) than VP-16 (IR, 60%) without loss of body weight. Unsaturated fatty acids could be evaluated to be good carrier vehicles of DDPT.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents, Phytogenic / administration & dosage
  • Antineoplastic Agents, Phytogenic / chemical synthesis
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Cells, Cultured / drug effects
  • Drug Carriers
  • Drug Screening Assays, Antitumor
  • Drugs, Chinese Herbal
  • Esters / administration & dosage
  • Esters / chemical synthesis
  • Esters / pharmacology*
  • Fatty Acids, Unsaturated / chemistry*
  • Mice
  • Podophyllotoxin / analogs & derivatives*
  • Podophyllotoxin / chemistry*

Substances

  • Antineoplastic Agents, Phytogenic
  • Drug Carriers
  • Drugs, Chinese Herbal
  • Esters
  • Fatty Acids, Unsaturated
  • deoxypodophyllotoxin
  • Podophyllotoxin