A reappraisal of the effect upon thymidine kinase of thymidine derivatives carrying large groups at the 5'-position

…, LC Davies, JA Stock, KR Harrap

Index: Barrie; Davies; Stock; Harrap Journal of Medicinal Chemistry, 1984 , vol. 27, # 8 p. 1044 - 1047

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Citation Number: 8

Abstract

Several thymidine derivatives with hydrophobic 5'-substituents, linked by chemically stable amide and ether links, were synthesized as potential thymidine kinase inhibitors. None of these was active nor were several derivatives of thymidine 5'-acetate, which were previously reported to be inhibitors. It was shown that the apparent inhibition by the latter compounds was due to their facile hydrolysis in aqueous solution with release of thymidine. These ...