We are currently investigating the synthesis of bimetallic complexes that are capable of binding DNA through intercalation at two different sites. Our efforts have focused on linking two Rh(phi)cyclen3+ (cyclen = 1,4,7,10-tetraazacyclododecane, phi = 9,10-diaminophenanthroline) intercalating groups through N-substituted cyclen ligands. Previously, Barton et al. established that the complex Rh(phi)cyclen3+ exhibited site specific DNA binding in the major groove for GC base pairs. To date our efforts have focused on two synthetic approaches: (i) direct alkylation of cyclen using dibromosubstituted organic spacers, and (ii) preparation of modified cyclen ligands bearing terminal alkynes that may be linked via double 1,3-dipolar cycloaddition reactions with diazo spacers. In both instances, we have first protected the cyclen spacer with glyoxal to allow for alkylation at a single N atom. A detailed account of the synthesis and characterization of these new ditopic ligands will be presented together with our efforts to incorporate Rh(phi)3+.

Design and synthesis of bimetallic DNA intercalators possessing two Rh(III) (9,10-diaminophenanthroline) groups

243rd National Meeting (2012)

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