期刊
CHEMISTRY-A EUROPEAN JOURNAL
卷 18, 期 35, 页码 10892-10902出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201200081
关键词
antitumor agents; DNA; G-quadruplexes; nucleophilic substitution; phenanthrolines
资金
- Danish Council for Independent Research, Technology and Production [274-08-056, 09-070364]
Small molecules capable of stabilizing the G-quadruplex (G4) structure are of interest for the development of improved anticancer drugs. Novel 4,7-diamino-substituted 1,10-phenanthroline-2,9-dicarboxamides that represent hybrid structures of known phenanthroline-based ligands have been designed. An efficient synthetic route to the compounds has been developed and their interactions with various G4 sequences have been evaluated by Forster resonance energy transfer (FRET) melting assays, fluorescent intercalator displacement (FID), electrospray ionization mass spectrometry (ESI-MS), and circular dichroism (CD) spectroscopy. The preferred compounds have high aqueous solubility and are strong and potent G4 binders with a high selectivity over duplex DNA; thus, they represent a significant improvement over the lead compounds. Two of the compounds are inhibitors of HeLa and HT1080 cell proliferation.
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