Prodrugs of biologically active phosphate esters

Research output: Contribution to journalArticlepeer-review

206 Scopus citations


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.

Original languageEnglish (US)
Pages (from-to)885-898
Number of pages14
JournalBioorganic and Medicinal Chemistry
Issue number6
StatePublished - Mar 2003
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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