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| - Synthesis and Biological Activity of Anticancer Ether Lipids That AreSpecifically Released by Phospholipase A2 in Tumor Tissue
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| - The clinical use of anticancer lipids is severely limited by their ability to cause lysis of redblood cells prohibiting intravenous injection. Novel delivery systems are therefore required inorder to develop anticancer ether lipids (AELs) into clinically useful anticancer drugs. In arecent article (J. Med. Chem. 2004, 47, 1694) we showed that it is possible to construct liposomesystems composed of masked AELs that are activated by secretory phospholipase A2 incancerous tissue. We present here the synthesis of six AELs and evaluate the biological activityof these bioactive lipids. The synthesized AEL 1−6 were tested against three different cancercell lines. It was found that the stereochemistry of the glycerol headgroup in AEL-2 and 3 hasa dramatic effect on the cytotoxicity of the lipids. AEL 1−4 were furthermore evaluated fortheir ability to prevent phosphorylation of the apoptosis regulating kinase Akt, and a correlationwas found between their cytotoxic activity and their ability to inhibit Akt phosphorylation.
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