5-diacetoxymethyl-cycloSal-d4TMP - A prototype of enzymatically activated cycloSal-pronucleotides.
A new class of "lock-in"-modified cycloSal-pronucleotides has been synthesized. On the example of 5-diacetoxymethyl-cycloSal-d4T-monophosphate (5-di-AM-cycloSal-d4TMP), the concept of enzymatically activated cycloSal-pronucleotides is elucidated. Synthesis, hydrolysis studies, and antiviral activities against HIV are presented.
Gisch
N
N
Department of Chemistry, Organic Chemistry, Faculty of Science, University of Hamburg, Martin-Luther-King-Platz 6, 20146 Hamburg, Germany. gisch@chemie.uni-hamburg.de
Balzarini
J
J
Meier
C
C
D004798:Enzymes / Q000378:metabolism*; D009711:Nucleotides / Q000378:metabolism*; D011355:Prodrugs / Q000378:metabolism*; D018119:Stavudine / Q000031:analogs & derivatives* / Q000378:metabolism; D013942:Thymine Nucleotides / Q000378:metabolism*
C526393:5-diacetoxymethyl-cyclosaligenyl-2',3'-didehydro-2',3'-dideoxythymidine; D004798:Enzymes; D009711:Nucleotides; D011355:Prodrugs; D013942:Thymine Nucleotides; D018119:Stavudine