Synthesis and evaluation of bis(imino)anthracene derivatives as G-quadruplex ligands

RSC Med Chem. 2021 Mar 26;12(5):751-757. doi: 10.1039/d0md00428f.

Abstract

The synthesis of a small number of bis(imino)anthracene derivatives is reported. They were evaluated via NMR for binding efficacy to the G-quadruplex-forming oligonucleotide sequence (TTGGGTT) and show activity against the HeLa cancer cell line. These novel ligands are compared to previously synthesised G-quadruplex ligands that target telomeres and oncogenes.