Biaryl polyamides as a new class of DNA quadruplex-binding ligands

摘要

We report a novel class of biaryl polyamides highly selective for G-quadruplex DNA, and with significant cytotoxicity in several cancer cell lines; they form planar U-shaped structures that match the surface area dimensions of a terminal G-quartet in quadruplex structures rather than the grooves of duplex DNA.rnGuanine-rich nucleic acid sequences can fold into four-stranded G-quadruplex structures. These structures may be adopted by telomeric DNA repeats as well as sequences in promoter and other regulatory regions within human and other genomes.