Open AccessNew insights regarding the potential of the pronucleotide approach in antiviral chemotherapy.
Author(s) -
Gilles Gosselin,
JeanLuc Girardet,
Christian Philouze,
S. Benzaria,
Isabelle Lefèbvre,
Nathalie Schlienger,
A. Pompon,
Jean−Louis Imbach
Publication year - 1996
Publication title -
acta biochimica polonica
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.452
H-Index - 78
eISSN - 1734-154X
pISSN - 0001-527X
DOI - 10.18388/abp.1996_4553
Subject(s) - chemistry , in vivo , enzyme , biochemistry , stereochemistry , combinatorial chemistry , pharmacology , computational biology , biology , microbiology and biotechnology
The rationale for a pronucleotide approach based on the use of phosphotriesters which incorporate enzyme-mediated bio-labile protection is discussed in detail. Among the studied bio-labile phosphate protecting groups, the S-acyl-2-thioethyl (SATE) groups appeared the most promising as exemplified in cell culture systems in the case of the pronucleotides of 3'-azido-3'-deoxythymidine, 2',3'-didehydro-3'-deoxythymidine, 2',3'-dideoxyadenosine and acyclovir In vivo implementations of such bis(SATE) pronucleotides have been planned for future animal studies.