"Lock-in" modified CycloSal nucleotides - The second generation of CycloSal prodrugs

Institute of Organic Chemistry, University of Hamburg, Hamburg, Germany.
Nucleosides Nucleotides &amp Nucleic Acids (Impact Factor: 1.02). 02/2005; 24(5-7):939-42. DOI: 10.1081/NCN-200059298
Source: PubMed


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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