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Bioorg Med Chem. 2003 Mar 20;11(6):885-98.

Prodrugs of biologically active phosphate esters.

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  • 1European Molecular Biology Laboratory, Meyerhofstr. 1, 69117, Heidelberg, Germany.


Bioactivatable protecting groups represent an enormously powerful tool to increase bioavailability or to generally help deliver drugs to cells. This approach is particularly valuable in the case of biologically active phosphates because of the high intrinsic hydrophilicity and the multitude of biological functions phosphate esters exhibit inside cells. Here, the most prominent masking groups used so far are introduced. The stability and toxicology of the resulting prodrugs is discussed. Finally, this review tries to cover briefly some of the work that describes the usefulness and efficiency of the approach in various application areas.

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