Synthesis and evaluation of a DHA and 10-hydroxycamptothecin conjugate

Bioorg Med Chem. 2005 Oct 1;13(19):5592-9. doi: 10.1016/j.bmc.2005.06.039.

Abstract

We have synthesized a conjugate of cis-4,7,10,13,16,19-docosahexenoic acid (DHA) and 10-hydroxycamptothecin (HCPT), DHA-HCPT. The antitumor activity of DHA-HCPT was evaluated in vitro against L1210 leukemia cells and in experimental animal tumor models including L1210 leukemia, Lewis lung carcinoma, and colon 38 adenocarcinoma. DHA-HCPT showed a greatly improved antitumor efficacy compared to HCPT.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adenocarcinoma / drug therapy*
  • Animals
  • Antineoplastic Agents* / chemical synthesis
  • Antineoplastic Agents* / pharmacology
  • Camptothecin / analogs & derivatives*
  • Camptothecin / chemical synthesis
  • Camptothecin / pharmacology
  • Carcinoma, Lewis Lung / drug therapy*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Colonic Neoplasms / drug therapy*
  • Disease Models, Animal
  • Docosahexaenoic Acids* / chemical synthesis
  • Docosahexaenoic Acids* / pharmacology
  • Drug Design
  • Drug Screening Assays, Antitumor
  • Humans
  • Leukemia L1210 / drug therapy*
  • Mice
  • Molecular Conformation
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • DHA-HCPT conjugate
  • Docosahexaenoic Acids
  • 10-hydroxycamptothecin
  • Camptothecin