Synthesis and activity of a folate peptide camptothecin prodrug

Walter A. Henne, Derek D. Doorneweerd, Andrew R. Hilgenbrink, Sumith A. Kularatne, Philip S. Low

Research output: Contribution to journalArticlepeer-review

132 Scopus citations


A folate receptor targeted camptothecin prodrug was synthesized using a hydrophilic peptide spacer linked to folate via a releasable disulfide carbonate linker. The conjugate was found to possess high affinity for folate receptor-expressing cells and inhibited cell proliferation in human KB cells with an IC50 of 10 nM. Activity of the prodrug was completely blocked by excess folic acid, demonstrating receptor-mediated uptake.

Original languageEnglish (US)
Pages (from-to)5350-5355
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Issue number20
StatePublished - Oct 15 2006


  • Camptothecin
  • Carbonate
  • Disulfide
  • Endocytosis
  • Folate
  • Folic acid
  • Peptide
  • Prodrug
  • Releasable linker
  • Targeted drug delivery

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science


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