Synthesis, characterization, DNA-binding and DNA-photocleavage studies of [Ru(bpy)2(pmip)]2+ and [Ru(phen)2(pmip)]2+ (pmip=2-(2′-pyrimidyl)imidazo[4,5-f][1,10]phenanthroline
摘要:
Two new Ru(II) complexes, [Ru(bpy)(2)(pmip)](2+) (1) and [Ru(phen)(2)(pmip)](2+) (2), have been synthesized and characterized by elemental analysis, ESI-MS and H-1 NMR spectra. Their DNA-binding properties were studied by means of UV-VIS, emission and CD spectra, thermal denaturation and viscosity measurements as well as their DNA-photocleavage properties. The experimental results show that both 1 and 2 can bind to DNA in an intercalative mode; the DNA-binding affinity of 2 is greater than that of 1, which suggests that the ancillary ligands have a significant effect on the spectroscopic properties and DNA-binding behavior of the Ru(II) complexes. Under irradiation with UV light, the Ru(II) complexes show excellent efficiency of cleaving DNA. This research may provide valuable insight into the interactions of metal complexes with DNA, knowledge that is an excellent backdrop for the rational design of promising drugs. (C) 2009 Elsevier Ltd. All rights reserved.
已经制备了一系列基于马参部分的新的Ru II Schiff碱复合物。其中包括四种包含Ni II,Pd II或Pt II的柔性单金属Ru II化合物和六个刚性双金属类似物阳离子进入丹参络合位点。稳态发光滴定表明该化合物具有光探针G-四链体(G4)DNA的能力。此外,席夫碱的大量结构变化允许广泛评估配体表面,柔性和电荷对化合物与G4 DNA相互作用的影响。这要归功于圆二色谱熔融分析和生物层干涉法研究,这些研究指出了Ru II Schiff碱基配合物对G4 DNA的高亲和力和良好的选择性。在纤维素用最有前途的化合物进行了研究。观察到化合物在核以及在核仁中的细胞摄取。在黑暗和光照射下,用U2OS骨肉瘤细胞进行细胞活力实验,从而可以测量IC 50值和光指数。他们显示了光照射除了在黑暗中分子的低细胞毒性外,还对药物的活性发挥了重要作用。总之,报告的结果强调了Ru II Schiff碱基复合物作为开发潜在的靶向诊断或治疗化合物的G4