High-affinity A/T-rich DNA binding with a dimeric bisbenzamidine

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Abstract A bisbenzamidine DNA binding agent can be easily dimerized by alkylation of its terminal amidine groups to afford an extended minor groove binder with over 20-fold enhanced DNA affinity towards extended A/T-rich sites. NMR experiments in combination with molecular dynamics simulation studies provide structural insight into the insertion of this compound in the DNA minor groove, and antimicrobial assays demonstrate that the increased affinity translates into higher antileishmanial activity.