Inactivation of O 6-alkylguanine-DNA alkyltransferase. 1. Novel O 6-(hetarylmethyl) guanines having basic rings in the side chain

…, J Kelly, AJ Watson, JA Rafferty, RH Elder…

Index: McElhinney; Donnelly; McCormick; Kelly; Watson; Rafferty; Elder; Middleton; Willington; McMurry; Margison Journal of medicinal chemistry, 1998 , vol. 41, # 26 p. 5265 - 5271

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Citation Number: 70

Abstract

A number of novel guanine derivatives containing heterocyclic moieties at the O 6-position have been synthesized using a purine quaternary salt which reacts with alkoxides under mild conditions. Initially O 6-substituents were investigated in which the benzene ring of the known agent, O 6-benzylguanine, was replaced by unsubstituted heterocyclic rings. The ability of these agents to inactivate the DNA repair protein O 6-alkylguanine-DNA ...