Platinum(II) Complexes with Dipyridophenazine Ligands as Human Telomerase Inhibitors and Luminescent Probes for G-Quadruplex DNA

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Abstract
A series of platinum(II) complexes containing dipyridophenazine (dppz) and C-deprotonated 2-phenylpyridine (N∧CH) ligands were prepared and assayed for G-quadruplex DNA binding activities. [PtII(dppz-COOH)(N∧C)]CF3SO3 (1; dppz-COOH = 11-carboxydipyrido[3,2-a:2′,3′-c]phenazine) binds G-quadruplex DNA through an external end-stacking mode with a binding affinity of ∼107 dm3 mol−1. G-quadruplex DNA binding is accompanied by up to a 293-fold increase in the intensity of photoluminescence at λmax = 512 nm. Using a biotinylated-primer extension telomerase assay, 1 was shown to be an effective inhibitor of human telomerase in vitro, with a telIC50 value of 760 nM.

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