| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374115 | Bioorganic & Medicinal Chemistry Letters | 2006 | 6 Pages |
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 IC50 of 10 nM. Activity of the prodrug was completely blocked by excess folic acid, demonstrating receptor-mediated uptake.
Graphical abstractThe synthesis and activity (IC50 = 10 nM) of a folate peptide camptothecin prodrug with a disulfide carbonate releasable linker is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Walter A. Henne, Derek D. Doorneweerd, Andrew R. Hilgenbrink, Sumith A. Kularatne, Philip S. Low,