Journal article
Synthesis and Biophysical Characterization of Chlorambucil Anticancer Ether Lipid Prodrugs
In
Journal of Medicinal Chemistry
—
2009, Volume 52, Issue 10, pp. 3408-3415
Abstract
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.
| Language: | English |
|---|---|
| Year: | 2009 |
| Pages: | 3408-3415 |
| ISSN: | 15204804 and 00222623 |
| Types: | Journal article |
| DOI: | 10.1021/jm900091h |
| ORCIDs: | Andresen, Thomas Lars , Madsen, Robert and Clausen, Mads Hartvig |
Keywords
