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.
Young-Jae You  1 ,  Yong Kim ,  Nguyen-Hai Nam ,  Byung-Zun Ahn
Affiliations
  • 1. College of Pharmacy, Chungnam National University, Taejon 305-764, South Korea.
PMID: 12873481 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.