Design and synthesis of labeled phospholipid ether analogs for biological evaluation.

摘要

A series of labeled phospholipid ether analogs was designed and synthesized as potential metabolic probes and tumor-specific imaging agents. These agents were designed to further understand the nature of the tumor-specific ether lipids.;A ;1-;Phosphatidylethanol is generated by the action of PLD in the presence of ethanol through a transphosphatidylation reaction. ;The stereospecificity of PLD was demonstrated using the unlabeled enantiomers of Et-18-;A series of halogenated ;Based on preliminary in vivo studies, the fluorinated agents appear to be either too toxic at current dosages, in the case of the dodecylphosphocholine analog, or entirely lacking in tumor-specificity, in the case of the heptylphosphocholine, Tissue distribution results using radioiodinated 7-(m-iodophenyl)heptylphosphocholine indicated that the seven carbon alkyl chain length is too short to be retained within tumors.