DESIGN AND SYNTHESIS OF G-QUADRUPLEX LIGANDS BEARING MACROCYCLIC HEXAOXAZOLES WITH FOUR-WAY SIDE CHAINS
DESIGN AND SYNTHESIS OF G-QUADRUPLEX LIGANDS BEARING MACROCYCLIC HEXAOXAZOLES WITH FOUR-WAY SIDE CHAINS
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DOI：
10.3987/com-11-s(p)88
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发表时间：
2012-01-01
期刊：
影响因子：
0.6
通讯作者：
Nagasawa, Kazuo
中科院分区：
文献类型：
--
作者：
Iida, Keisuke;Majima, Satoki;Nagasawa, Kazuo
合成了具有四元侧链的大环六恶唑类化合物L_2H_2-（4 M）_6OTD衍生物3和4。通过FRET（荧光共振能量转移）测定评价了这些化合物对人端粒、c-kit、bcl-2和c-myc中的G-四链体形成寡核苷酸的稳定性。这些化合物与具有双向侧链L2 H2-（4 M）6 OTD（2d）的配体相比显示出较低的稳定能力。
Macrocyclic hexaoxazole compounds bearing four-way side chains L2H2-(4M)6OTD derivatives 3 and 4 were synthesized as new G-quadruplex ligands. Stabilization of G-quadruplex forming oligonucleotides in human telomeres, c-kit, bcl-2, and c-myc with those compounds was evaluated by the FRET (fluorescence resonance energy transfer) assay. These compounds showed less stabilizing ability compared to the ligand possessing two-way side chain of L2H2-(4M)6OTD (2d).