Tri- and tetra-substituted naphthalene diimides as potent G-quadruplex ligands
Tri- and tetra-substituted naphthalene diimides as potent G-quadruplex ligands
复制标题
DOI：
10.1016/j.bmcl.2008.01.050
复制
发表时间：
2008-03-01
影响因子：
2.7
通讯作者：
Neidle, Stephen
中科院分区：
文献类型：
--
作者：
Cuenca, Francisco;Greciano, Olga;Neidle, Stephen
设计并合成了一系列三取代和四取代萘二亚胺。在经典和竞争FRET测定和SPR研究中，一些化合物显示出对端粒g -四重体DNA的特殊亲和力。在TRAP实验中，它们抑制端粒酶，并对MCF7和A549癌细胞系显示出有效的基于衰老的短期抗增殖作用，并且定位于MCF7细胞的细胞核，特别是核心区。(c) 2008 Elsevier Ltd.版权所有。
A series of tri- and tetra-substituted naphthalene diimides have been designed and synthesized. Several compounds show exceptional affinity for telomeric G-quadruplex DNA in classical and competition FRET assays and SPR studies. They inhibit telomerase in the TRAP assay, and show potent senescence-based short-term anti-proliferative effects on MCF7 and A549 cancer cell lines, and localize in the nucleus and particularly the nucleolus of MCF7 cells. (c) 2008 Elsevier Ltd. All rights reserved.