Synthesis and evaluation of 9-O-substituted berberine derivatives containing aza-aromatic terminal group as highly selective telomeric G-quadruplex stabilizing ligands
Synthesis and evaluation of 9-O-substituted berberine derivatives containing aza-aromatic terminal group as highly selective telomeric G-quadruplex stabilizing ligands
复制标题
含氮杂芳香端基的 9-O-取代小檗碱衍生物作为高选择性端粒 G-四链体稳定配体的合成与评价
DOI：
10.1016/j.bmcl.2009.05.030
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发表时间：
2009-07-01
影响因子：
2.7
通讯作者：
Huang, Zhi-Shu
中科院分区：
文献类型：
--
作者：
Ma, Yan;Ou, Tian-Miao;Huang, Zhi-Shu
合成了一系列新的9-O-取代小檗碱衍生物（4a-j）作为调聚四链体配体。生物物理和生物化学实验结果表明，在小檗碱9位侧链上引入带正电荷的氮杂芳香末端基团，可显著提高小檗碱与G-四链体的结合能力，并对杂交和端粒酶活性有抑制作用。这些衍生物对端粒G-四链体DNA的选择性优于双链体。(C)2009爱思唯尔有限公司版权所有。
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. (C) 2009 Elsevier Ltd. All rights reserved.