Antitumor phosphate-containing lipids and non-phosphorus alkyl cationic glycerolipids: Chemical structures and perspectives of drug development

Candidates to antitumor drugs of lipid nature are reviewed. The biological effects of the following known antineoplastic phosphate-containing lipids are described: edelfosine, ilmofosine, milfosine, perifosine, and erufosine. Although the most active phosphate-containing lipid edelfosine causes the death of tumor cells of different tissue origin, it possesses a strong hemolytic effect and toxicity toward non-malignant counterparts. The phosphate-containing lipids can be inactivated by phospholipases, which gave rise to the search for the optimum structure of cationic glycerolipids containing no phosphate group and having a similar antitumor activity. The results of structural functional studies of the non-phosphorus cationic glycerolipids with the best antitumor activity are generalized.