Synthesis and activity of a folate peptide camptothecin prodrug
The synthesis and activity (IC 50 = 10 nM) of a folate peptide camptothecin prodrug with a disulfide carbonate releasable linker is reported. A folate receptor targeted camptothecin prodrug was synthesized using a hydrophilic peptide spacer linked to folate via a releasable disulfide carbonate linke...
Gespeichert in:
Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2006-10, Vol.16 (20), p.5350-5355 |
---|---|
Hauptverfasser: | , , , , |
Format: | Artikel |
Sprache: | eng |
Schlagworte: | |
Online-Zugang: | Volltext |
Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
Zusammenfassung: | The synthesis and activity (IC
50
=
10
nM) of a folate peptide camptothecin prodrug with a disulfide carbonate releasable linker is reported.
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 10
nM. Activity of the prodrug was completely blocked by excess folic acid, demonstrating receptor-mediated uptake. |
---|---|
ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2006.07.076 |