Abstract
A series of new 9-O-substituted berberine derivatives (4a-j) as telomeric quadruplex ligands was synthesized and evaluated. The results from biophysical and biochemical assay indicated that introducing of positive charged aza-aromatic terminal group into the side chain of 9-position of berberine significantly improved the binding ability with G-quadruplex, and exhibited the inhibitory effect on the hybridization and on telomerase activity. These derivatives showed excellent selectivity for telomeric G-quadruplex DNA over duplex.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Aza Compounds / chemistry*
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Berberine / analogs & derivatives*
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Berberine / chemical synthesis
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Berberine / pharmacology
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Cell Line, Tumor
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Fluorescence Resonance Energy Transfer
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G-Quadruplexes*
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Humans
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Ligands
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Reverse Transcriptase Inhibitors / chemical synthesis*
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Reverse Transcriptase Inhibitors / chemistry
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Reverse Transcriptase Inhibitors / pharmacology
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Telomerase / antagonists & inhibitors*
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Telomerase / metabolism
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Telomere / chemistry*
Substances
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Aza Compounds
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Ligands
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Reverse Transcriptase Inhibitors
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Berberine
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Telomerase