Study of different substituted cyclic and acyclic benzylpronucleotides of d4T relative to their hydrolytic stability and antiviral activity

…, E De Clercq, J Balzarini, L Naesens…

Index: Muus; De Clercq; Balzarini; Naesens; Meier Nucleosides, Nucleotides and Nucleic Acids, 2003 , vol. 22, # 5-8 p. 791 - 795

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Abstract

Abstract Cyclo Sal-d4TMP and two different bis (benzyl) phosphate triesters of the antivirally active nucleoside analog d4T were studied with regard to their chemical hydrolysis behavior at pH 7.3, in CEM/0 cell extracts, and their anti-HIV activity. In contrast to triesters 2–4, bis-(o- AB)-d4TMP 1 was found to be chemically exquisitely stable. All compounds led to the formation of d4TMP in cell extracts and all triesters achieved the TK-bypass.