Synthesis and Biophysical Testing of a Novel Pyrrole-Containing Polyamide-Benzamidine Hybrid

Abstract

This communication details the rationale for the design of a novel polyamide molecule, 1, in which the standard dimethylamino C-terminus functionality has been replaced with a benzamidine moiety. The synthesis of this molecule and the subsequent DNA binding properties, determined from surface plasmon resonance and DNA melts are reported. The benzamidine moiety was shown to significantly increase the binding affinity of the polyamide to its cognate AATTT sequence compared to the parent C-terminus compound 2.