Through the derivatization of azobenzene and indigo-based dyes, a small library of G-quadruplex ligands was synthesized and characterized. Compounds with various tertiary amine side chains were synthesized in 2-3 steps in good yields. Moderate G-quadruplex stabilization, as measured by changes in DNA melting curves, was achieved with several compounds. These dye derivatives represent new core structures that have G-quadruplex stabilizing properties and the potential for novel anticancer therapies.

Synthesis and evaluation of dye derivatives as G-quadruplex-stabilizing molecules

253rd National Meeting (2017)

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