Synthesis and evaluation of 9-O-substituted berberine derivatives containing aza-aromatic terminal group as highly selective telomeric G-quadruplex stabilizing ligands |
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Authors: | Yan Ma Tian-Miao Ou Jia-Heng Tan Jin-Qiang Hou Shi-Liang Huang Lian-Quan Gu Zhi-Shu Huang |
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Affiliation: | School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, People’s Republic of China |
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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. |
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