Tetrasubstituted naphthalene diimide ligands with selectivity for telomeric G-quadruplexes and cancer cells.

Hampel, Sonja M, Sidibe, Assitan, Gunaratnam, M., Riou, Jean-Francois and Neidle, S. (2010) Tetrasubstituted naphthalene diimide ligands with selectivity for telomeric G-quadruplexes and cancer cells. Bioorganic & Medicinal Chemistry Letters, 20 (22). pp. 6459-63. 10.1016/j.bmcl.2010.09.066 .

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DOI: 10.1016/j.bmcl.2010.09.066

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.

Item Type:Article
Uncontrolled Keywords:Quadruplex; Naphthalene diimide; Telomerase; Cancer
Departments, units and centres:Department of Pharmaceutical and Biological Chemistry > Cancer Research UK Biomolecular Structure Group
ID Code:1784
Journal or Publication Title:Bioorganic & Medicinal Chemistry Letters
Deposited By:Library Staff
Deposited On:18 Feb 2011 17:30
Last Modified:11 Nov 2011 16:32

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