Synthesis and evaluation of 9-O-substituted berberine derivatives containing aza-aromatic terminal group as highly selective telomeric G-quadruplex stabilizing ligands

被引：77

作者：

Ma, Yan ^{[1
]}

Ou, Tian-Miao ^{[1
]}

Tan, Jia-Heng ^{[1
]}

Hou, Jin-Qiang ^{[1
]}

Huang, Shi-Liang ^{[1
]}

Gu, Lian-Quan ^{[1
]}

Huang, Zhi-Shu ^{[1
]}

机构：

[1] Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510275, Guangdong, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 13期

关键词：

G-Quadruplex; Berberine derivatives; Selectivity; Telomerase inhibitors; ANTITUMOR POLYCYCLIC ACRIDINES; ANTIMICROBIAL ACTIVITY; CATIONIC PORPHYRINS; CELL-PROLIFERATION; BINDING; DNA; TELOMESTATIN; INHIBITORS; AGENTS;

D O I：

10.1016/j.bmcl.2009.05.030

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：3414 / 3417

页数：4