Synthesis, hydrolysis and anti-EBV activity of a series of 3'-modified cycloSal-BVDUMP pronucleotides.
A series of cycloSal-BVDUMP phosphate triesters has been prepared. The prototype compound was 3-methyl-cycloSal-BVDUMP 2. Furthermore, a series of 3'-O-acyl-modified derivatives having carboxylic acids with different lipophilicity or a L-configurated alpha-amino acid (phenylalanine) was prepared. The hydrolysis properties in phosphate buffer PBS as well as in PBS containing pig liver esterase (PLE) will be described. Finally, the biological activity against EBV has been determined.
Meier
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C
University of Hamburg, Institute of Organic Chemistry, Martin-Luther-King-Platz 6, D 20146 Hamburg, Germany.
Lomp
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A
Meerbach
A
A
Wutzler
P
P
D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001973:Bromodeoxyuridine / Q000031:analogs & derivatives*; D002460:Cell Line; D004854:Herpesvirus 4, Human / Q000187:drug effects*; D006801:Humans; D006868:Hydrolysis; D008214:Lymphocytes / Q000821:virology; D008826:Microbial Sensitivity Tests; D009711:Nucleotides / Q000138:chemical synthesis* / Q000494:pharmacology*
D000998:Antiviral Agents; D009711:Nucleotides; D001973:Bromodeoxyuridine