Bis-intercalative binding to DNA of novel bis(10-methyl)acridinium chlorides and its dependence on chain length of linker

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Abstract
The synthesis of a series of novel bis(10-methyl)acridinium compounds (both unsubstituted and the 6-chloro-2-methoxy substituted) linked by methylene bridges of lengths from (CH2)4 to (CH2)12 and in one case by spermine is described. Their ability to bind to duplex DNA was compared by their relative inhibition of Escherichia coli DNA polymerase catalyzed DNA synthesis. It was determined that they function as DNA template inhibitors and do not affect the DNA polymerase directly. Their ability to function as bis-intercalators was assessed by a novel and convenient [calf thymus] topoisomerase fluorescent assay. Whereas the (CH2)4-linked compounds act only as monofunctional intercalators because of steric constraints the (CH2)6-, (CH2)8- and (CH2)10-linked substituted bisacridinium compounds, as well as the (CH2)10- and (CH2)12-unsubstituted analogs, probably function as bis-intercalators with DNA.

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