Issue 8, 2011

Promoting the formation and stabilization of human telomeric G-quadruplex DNA, inhibition of telomerase and cytotoxicity by phenanthroline derivatives

Abstract

Four new di-substituted phenanthroline-based compounds a–d have been designed and prepared, and they have been shown to induce the formation of anti-parallel structure of human telomeric G-quadruplex DNA by CD spectra. FRET assay indicates that the melting temperature increases (ΔTm values) of G-quadruplex in buffer (pH 7.4) containing 100 mM NaCl are 31.6, 34.6, 17.8 and 32.6 °C for the compounds (1.0 μM) a, b, c and d, respectively. Competitive FRET assay shows that the four compounds exhibit a high G-quadruplex DNA selectivity over duplex DNA. Three of the compounds are the potent telomerase inhibitors and HeLa cell proliferation inhibitors.

Graphical abstract: Promoting the formation and stabilization of human telomeric G-quadruplex DNA, inhibition of telomerase and cytotoxicity by phenanthroline derivatives

Supplementary files

Article information

Article type
Paper
Submitted
01 Nov 2010
Accepted
12 Jan 2011
First published
12 Jan 2011

Org. Biomol. Chem., 2011,9, 2648-2653

Promoting the formation and stabilization of human telomeric G-quadruplex DNA, inhibition of telomerase and cytotoxicity by phenanthroline derivatives

L. Wang, Y. Wen, J. Liu, J. Zhou, C. Li and C. Wei, Org. Biomol. Chem., 2011, 9, 2648 DOI: 10.1039/C0OB00961J

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