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ID: ALA1137292

Journal: Bioorg Med Chem Lett

Title: Synthesis and activity of a folate peptide camptothecin prodrug.

Authors: Henne WA, Doorneweerd DD, Hilgenbrink AR, Kularatne SA, Low PS.

Abstract: 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 IC(50) of 10nM. Activity of the prodrug was completely blocked by excess folic acid, demonstrating receptor-mediated uptake.

CiteXplore: 16901694

DOI: 10.1016/j.bmcl.2006.07.076