手性钌配合物Δ-[Ru(bpy)_2IPBP]^(2+)的合成及其细胞毒作用

Studies on the synthesis and cytotoxicity of chiral ruthenium(II) complex Δ-[Ru(bpy)_2IPBP]^(2+)

目的采用Δ-[Ru(bpy)2(py)2][o,o′-dibenzoyltartrate].12H2O和3-醛基色酮为原料,制备手性钌多吡啶配合物Δ-[Ru(bpy)2IPBP]2+(Δ-1)(bpy=bipyridine,IPBP=2-(4-甲苯并吡喃-2-酮)咪唑[4,5-f][1,10]菲咯啉),并对其体外抗肿瘤活性进行初步评价。方法采用元素分析,电喷雾质谱(ESI-MS),核磁共振(NMR)等对目标化合物进行了表征,并采用MTT法初步研究了配合物Δ-1对人肝癌细胞Bel-7402,肺腺癌细胞HCT-8有明显的抑制作用。结果与结论目标化合物的元素分析、电喷雾质谱实验结果与理论值基本一致;当配合物浓度为50μg/mL时,配合物Δ-1对人肝癌细胞Bel-7402,肺腺癌细胞HCT-8有明显的抑制作用。

Objective To preparation a novel chiral ruehtnium （Ⅱ） complexes, △- [ Ru （bpy） 2IPBP ] ^2＋ （ △-1 ） （ bpy = bipyridine, IPBP =2-（4-methy-l-benzopyran） imidazo [4,5-f] [ 1,10] phenanthroline） and evaluate its antitumor activity. Methods The target compound △-1 was synthesized and characterized by elementary analysis, ESI-MS and 1H NMR, and the cytotoxicity of this ruthenium （Ⅱ） complex △-1 against human hepatocarcinoma cell line Bel-7402 and human intestinal adenocarcinoma cell line HCT-8 and human lung adenocarcinoma epithelial cell line A-549 were also investigated by MTT methods. Results and conclusion The studies showed that △-1 exhibited excellent antitumor activities against Bel-7402 hepatocarcinoma ceils and HCT-8 intestinal adenocarcinoma ceils at dose of 50 μg/mL,