Lysinyl macrocyclic hexaoxazoles: Synthesis and selective G-quadruplex stabilizing properties
Lysinyl macrocyclic hexaoxazoles: Synthesis and selective G-quadruplex stabilizing properties
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DOI：
10.1016/j.bmcl.2007.12.048
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发表时间：
2008-02-01
影响因子：
2.7
通讯作者：
Rice, Joseph E.
中科院分区：
文献类型：
--
作者：
Rzuczek, Suzanne G.;Pilch, Daniel S.;Rice, Joseph E.
已经合成了具有一个或两个赖氨酰基侧链的大环六恶唑，其中末端氮是伯胺、N，N-二甲胺或乙酰胺。已发现钠离子通过充当线性聚恶唑可围绕其组织的模板而有益于大环化步骤。每种靶向化合物选择性稳定G-四链体相对于双链体DNA。具有一个缬氨酸和一个赖氨酸残基的化合物显示出G-四链体稳定能力的最佳组合，而没有可检测到的双链体DNA的稳定。(C)2007爱思唯尔有限公司保留所有权利。
Macrocyclic hexaoxazoles having one or two lysinyl side chains in which the terminal nitrogen is either a primary amine, N,N-dimethylamine, or an acetamide have been synthesized. Sodium ion has been found to be beneficial to the macrocyclization step by acting as a template around which the linear polyoxazole can organize. Each of the targeted compounds selectivity stabilizes G-quadruplex versus duplex DNA. Compounds with one valine and one lysine residue display the best combination of G-quadruplex stabilizing ability with no detectable stabilization of duplex DNA. (C) 2007 Elsevier Ltd. All rights reserved.