Asymmetric derivatives of furamidines with one of the phenyl rings of
furamidine replaced with a benzimidazole have been found by quantitative
footprinting analyses to bind GC containing sites on DNA more strongly
than to pure AT sequences. These compounds have been shown to bind in the
minor groove at specific GC containing sequences of DNA in a highly
cooperative manner as a stacked dimer. Compounds of the present invention
find use in selectively binding mixed sequence DNA, and may also be used
in methods of regulating gene expression, methods of treating
opportunistic infections and cancer, as well as in methods of detecting
certain sequences of DNA.