“LOCK-IN” MODIFIED CYCLOSAL NUCLEOTIDES—THE SECOND GENERATION OF CYCLOSAL PRODRUGS

D. Vukadinović Institute of Organic Chemistry, University of Hamburg, Hamburg, Germany

N. P. H. Böge Institute of Organic Chemistry, University of Hamburg, Hamburg, Germany

J. Balzarini Rega Institute for Medical Research, Katholieke Universiteit, Leuven, Belgium

C. Meier Institute of Organic Chemistry, University of Hamburg, Hamburg, Germany

Abstract

A new generation of cycloSal-pronucleotides is presented. CycloSal-d4TMPs have been modified by introduction of an esterase-cleavable site in order to trap them inside cells. Hydrolysis studies in different media (PBS, CEM/0- and liver extracts) and anti-HIV evaluation of separated diastereomers revealed unexpected differences between the isomers.

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“LOCK-IN” MODIFIED CYCLOSAL NUCLEOTIDES—THE SECOND GENERATION OF CYCLOSAL PRODRUGS

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“LOCK-IN” MODIFIED CYCLOSAL NUCLEOTIDES—THE SECOND GENERATION OF CYCLOSAL PRODRUGS

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