Effects of intercalative ligands on the DNA binding, DNA topoisomerase II and DNA transcription inhibition of polypyridyl ruthenium(II) complexes
Effects of intercalative ligands on the DNA binding, DNA topoisomerase II and DNA transcription inhibition of polypyridyl ruthenium(II) complexes
复制标题
插入配体对聚吡啶钌(II)配合物DNA结合、DNA拓扑异构酶II和DNA转录抑制的影响
DOI：
10.1016/j.ica.2011.08.047
复制
发表时间：
2011-11-30
影响因子：
2.8
通讯作者：
Ji, Liang-Nian
中科院分区：
文献类型：
--
作者：
Chen, Xing;Gao, Feng;Ji, Liang-Nian
为了研究插入配体对其生物活性的影响，五个新配合物 [Ru(bpy)(2)(dpq)](ClO4)(2) (bpy = 2,2'-联吡啶，dpq = 二吡啶并喹喔啉)、[Ru(bpy)(2)(dicnq)](ClO4)(2) (dicnq =吡嗪并[2,3-f]菲咯啉-2,3-二甲腈)、[Ru(bpy)(2)(dppp3)](ClO4)(2) (dppp3 = 吡啶并[3',4':5,6]吡嗪并[2,3-f][1,10]菲咯啉)、[Ru(bpy)(2)(dppp2)](ClO4)(2) (dppp2 = 吡啶并[2',3':5,6]吡嗪基[2,3-f][1,10]菲咯啉) 和 [Ru(bpy)(2)(OCH3-dppz)](ClO4)(2) (OCH3-dppz = 11-甲氧基-联吡啶[3,2-a:2',3'-c]吩嗪) 已通过 H-1 合成并详细表征核磁共振波谱、质谱和元素分析。它们与小牛胸腺 DNA 的相互作用以及对拓扑异构酶 II 和 T7 RNA 聚合酶的抑制活性已通过一系列实验方法进行了检测。结果表明，高 DNA 结合亲和力对于拓扑异构酶 II 和 DNA 转录抑制非常重要。具有更大芳香区域、更好的共轭效应和吸电子取代基的插入配体有利于其多吡啶基Ru(II)配合物的DNA插入和酶抑制。 (C) 2011 Elsevier B.V. 保留所有权利。
To investigate the effect of intercalative ligand on their biological activity, five new complexes [Ru(bpy)(2)(dpq)](ClO4)(2) (bpy = 2,2'-bipyridine, dpq = dipyridoquinoxaline), [Ru(bpy)(2)(dicnq)](ClO4)(2) (dicnq = pyrazino[2,3-f]phenanthroline-2,3-dicarbonitrile), [Ru(bpy)(2)(dppp3)](ClO4)(2) (dppp3 = pyrido [3',4':5,6]pyrazino[2,3-f][1,10]phenanthroline), [Ru(bpy)(2)(dppp2)](ClO4)(2) (dppp2 = pyrido[2',3':5,6]pyrazino[2,3-f][1,10]phenanthroline) and [Ru(bpy)(2)(OCH3-dppz)](ClO4)(2) (OCH3-dppz = 11-methoxy-dipyrido[3,2-a:2',3'-c]phenazine) have been synthesized and characterized in detail by H-1 NMR spectroscopy, mass spectrometry and elemental analysis. Their interaction with calf thymus DNA and the inhibitory activity towards topoisomerase II and T7 RNA polymerase have been examined by a series of experimental methods. The results suggest that a high DNA-binding affinity is important for their topoisomerase II and DNA transcription inhibition. Intercalative ligands with more extended aromatic area, better conjugate effect and presence of electron-withdrawing substituted groups are beneficial to the DNA intercalation and enzymatic inhibition of their polypyridyl Ru(II) complexes. (C) 2011 Elsevier B.V. All rights reserved.