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Updated: Jun 8, 2026

In Vitro Chemical Mapping of G-Quadruplex DNA Structures by Bis-3-Chloropiperidines
Published on: May 12, 2023
Tetrasubstituted naphthalene diimide ligands with selectivity for telomeric G-quadruplexes and cancer cells
Sonja M Hampel1, Assitan Sidibe, Mekala Gunaratnam
1CRUK Biomolecular Structure Group, The School of Pharmacy, University of London, London WC1N 1AX, UK.
Abstract:
A series of tetrasubstituted naphthalene diimide compounds with N-methylpiperazine end groups has been synthesized and evaluated as G-quadruplex ligands. They have high affinity and selectivity for telomeric G-quadruplex DNA over duplex DNA. CD studies show that they induce formation of a parallel G-quadruplex topology. They inhibit the binding of hPOT1 and topoisomerase IIIα to telomeric DNA and inhibit telomerase activity in MCF7 cells. The compounds have potent activity in a panel of cancer cell lines, with typical IC(50) values of ∼0.1 μM, and up to 100-fold lower toxicity in a normal human fibroblast cell line.
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