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ChemMedChem. 2012 Jan 2;7(1):85-94. doi: 10.1002/cmdc.201100453. Epub 2011 Nov 3.

Platinum(II) phenanthroimidazoles for targeting telomeric G-quadruplexes.

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Department of Chemistry, McGill University, Montreal, QC, Canada.


A rationally designed progression of phenanthroimidazole platinum(II) complexes were examined for their ability to target telomere-derived intramolecular G-quadruplex DNA. Through the use of circular dichroism, fluorescence displacement assays, and molecular modeling we show that these complexes template and stabilize G-quadruplexes from sequences based on the human telomeric repeat (TTAGGG)(n). The greatest stabilization was observed for the p-chlorophenyl derivative 6((G4)DC(50) =0.31 μM). We also show that the G-quadruplex binding complexes are able to inhibit telomerase activity through a modified telomerase repeat amplification protocol (TRAP-LIG assay). Preliminary cell studies show that complex 6 is preferentially cytotoxic toward cancer over normal cell lines, indicating its potential use in cancer therapy.

[Indexed for MEDLINE]

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