Synthesis and Biophysical Characterization of Chlorambucil Anticancer Ether Lipid Prodrugs

Palle Jacob Pedersen, Mikkel Stochkendahl Christensen, Tristan Ruysschaert, Lars Linderoth, Thomas Lars Andresen, Fredrik Melander, Ole G. Mouritsen, Robert Madsen, Mads Hartvig Clausen

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The synthesis and biophysical characterization of four prodrug ether phospholipid conjugates are described. The lipids are prepared from the anticancer drug chlorambucil and have C16 and C18 ether chains with phosphatidylcholine or phosphatidylglycerol headgroups. All four prodrugs have the ability to form unilamellar liposomes (86-125 nm) and are hydrolyzed by phospholipase A2, resulting in chlorambucil release. Liposomal formulations of prodrug lipids displayed cytotoxicity toward HT-29, MT-3, and ES-2 cancer cell lines in the presence of phospholipase A2, with IC50 values in the 8-36 μM range.
Original languageEnglish
JournalJournal of Medicinal Chemistry
Issue number10
Pages (from-to)3408-3415
Publication statusPublished - 2009


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