Abstract

A series of bisubstrate inhibitors for DNA N6 adenine methyltransferase (Dam) have been synthesized by linking an amine analogue of S-adenosylmethionine to an aryl moiety designed to probe the binding pocket of the DNA adenine base. An initial structure–activity relationship study has identified substituents that increase inhibitor potency to the ∼10μM range and improve selectivity against the human cytosine methyltransferase Dnmt1.

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