Constrained bisantrene derivatives as G-quadruplex binders

Abstract

We here report the synthesis and evaluation of constrained derivatives of a bisantrene isomer known to bind DNA when structured in G-quadruplex. Enhanced high-resolution mass spectrometry was used to evaluate the binding efficiency and stoichiometry of the compounds towards G-quadruplex DNA using a duplex sequence for comparison. Fluorimetric DNA binding studies supported and confirmed these preliminary observations. One of the newly synthesized compounds showed a high tendency and specificity to bind the structured G-quadruplex DNA.