含三个侧链的大环六氧杂唑的合成及端粒 G-四链体稳定能力。
Synthesis and Telomeric G-Quadruplex-Stabilizing Ability of Macrocyclic Hexaoxazoles Bearing Three Side Chains.
机构信息
Department of Biotechnology and Life Science, Tokyo University of Agriculture and Technology, 2-24-16 Naka-cho, Koganei, Tokyo 184-8588, Japan.
Department of Chemistry, Chiba University, 1-33 Yayoi, Inage, Chiba 263-8522, Japan.
出版信息
Molecules. 2019 Jan 11;24(2):263. doi: 10.3390/molecules24020263.
G-quadruplexes (G4s), which are structures formed in guanine-rich regions of DNA, are involved in a variety of significant biological functions, and therefore "sequence-dependent" selective G4-stabilizing agents are required as tools to investigate and modulate these functions. Here, we describe the synthesis of a new series of macrocyclic hexaoxazole-type G4 ligand (6OTD) bearing three side chains. One of these ligands, , stabilizes telomeric G4 preferentially over the G4-forming DNA sequences of and , due to the interaction of its piperazinylalkyl side chain with the groove of telomeric G4.
G-四链体（G4s）是在富含鸟嘌呤的 DNA 区域形成的结构，参与多种重要的生物学功能，因此需要“序列依赖性”选择性 G4 稳定剂作为研究和调节这些功能的工具。在这里，我们描述了一系列带有三个侧链的新型大环六氧杂唑型 G4 配体（6OTD）的合成。其中一种配体 ，由于其哌嗪烷基侧链与端粒 G4 沟的相互作用，优先稳定端粒 G4，而不是 G4 形成的 DNA 序列 和 。
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