期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 9, 期 8, 页码 2648-2653出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c0ob00961j
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资金
- National Natural Science Foundation of China [21041008]
- Shanxi Provincial Fund for Natural Sciences [2009011012-2]
- Shanxi Scholarship Council of China
- Innovation Foundation for Shanxi Graduate students of China
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 (Delta T-m values) of G-quadruplex in buffer (pH 7.4) containing 100 mM NaCl are 31.6, 34.6, 17.8 and 32.6 degrees C for the compounds (1.0 mu M) 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.
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