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

Ma, Dik-Lung, Che, Chi-Ming, Yan, Siu-Cheong·2009·Journal of the American Chemical Society

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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 approximately 10(7) dm3 mol-1. G-quadruplex DNA binding is accompanied by up to a 293-fold increase in the intensity of photoluminescence at lambdamax = 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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See all 289

Authors: Ma, D.-L., Che, C.-M., & Yan, S.-C.
Venue: Journal of the American Chemical Society
Publisher: American Chemical Society (ACS)
Published: 2008-11-08
Volume: 131
Issue: 5
Pages: 1835-1846
ISSN: 0002-7863 (ISSN-L)
1520-5126
DOI: 10.1021/ja806045x
OpenAlex: W2026950328
Cited by: 289
References: 71
FWCI: 12.17
Type: journal article
Language: en
Open access: closed

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

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