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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