4.1 Article Proceedings Paper

SATE (aryl) phosphotriester series. II. Stability studies and physicochemical parameters

Journal

NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS
Volume 22, Issue 5-8, Pages 907-909

Publisher

MARCEL DEKKER INC
DOI: 10.1081/NCN-120022683

Keywords

LC/MS; prodrug; mononucleolide; AZT

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The stability of phosphotriester derivatives of 3'-azido-2',3'-dideoxythymidine (AZT) bearing a S-pivaloyl-2-thioethyl (tBuSATE) group and various aryl residues derived from L-tyrosine was evaluated in biological media. The results demonstrate that such compounds give rise to intracellular delivery of the parent mononucleotide through esterase and phosphodiesterase hydrolytic steps, successively.

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