作为高效G-四链体配体的三取代和四取代萘二亚胺
Tri- and tetra-substituted naphthalene diimides as potent G-quadruplex ligands.
作者信息
Cuenca Francisco, Greciano Olga, Gunaratnam Mekala, Haider Shozeb, Munnur Deeksha, Nanjunda Rupesh, Wilson W David, Neidle Stephen
机构信息
CRUK Biomolecular Structure Group, The School of Pharmacy, University of London, 29/39 Brunswick Square, London WC1N 1AX, UK.
出版信息
Bioorg Med Chem Lett. 2008 Mar 1;18(5):1668-73. doi: 10.1016/j.bmcl.2008.01.050. Epub 2008 Jan 18.
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.
一系列三取代和四取代的萘二亚胺已被设计并合成。在经典和竞争荧光共振能量转移（FRET）分析以及表面等离子体共振（SPR）研究中，几种化合物对端粒G-四链体DNA表现出非凡的亲和力。它们在端粒重复扩增法（TRAP）分析中抑制端粒酶，并对MCF7和A549癌细胞系表现出基于衰老的强效短期抗增殖作用，且定位于MCF7细胞的细胞核，尤其是核仁。
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