Isosteres of nucleoside triphosphates

R Weaver, IH Gilbert, N Mahmood, J Balzarini

Index: Weaver, Richard; Gilbert, Ian H.; Mahmood, Naheed; Balzarini, Jan Bioorganic and Medicinal Chemistry Letters, 1996 , vol. 6, # 20 p. 2405 - 2410

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Citation Number: 12

Abstract

Introduction All current antiviral nucleosides, such as AZT, d4T, acyclovir and BVDU are activated intracellularly by phosphorylation to the bioactive triphosphate form. The activation uses either the human kinases (eg in the case of HIV) or viral kinases (eg in the case of HSV). In some cases this intracellular activation is slow because the nucleosides are not good substrates of the kinases. For example in the case of d4T the phosphorylation of the nucleoside is the rate ...