Some 6-aza-5-substituted-2′-deoxyuridines show potent and selective inhibition of herpes simplex virus type 1 thymidine kinase

…, F Focher, A Verri, S Spadari, B Wroblowski…

Index: Basnak; Sun; Hamor; Focher; Verri; Spadari; Wroblowski; Herdewijn; Walker Nucleosides and Nucleotides, 1998 , vol. 17, # 1-3 p. 187 - 206

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Citation Number: 18

Abstract

Abstract The synthesis and X-ray crystal structures of a series of 5-substituted-6-aza-2′- deoxyuridines is reported. These nucleoside analogues inhibit the phosphorylation of thymidine by HSV-1 TK but have no effect on the corresponding human enzyme. Detailed examination of one analogue proves it to be a competitive inhibitor of thymidine with a Ki of 0.34 μM and is a very poor substrate. The analogues are not substrates for the enzyme ...