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Cytotoxic Activity of Some Half-sandwich Rhodium(III) Complexes Containing 4,4’-disubstituted-2,2’-bipyridine Ligands
Zeitschrift für anorganische und allgemeine Chemie ( IF 1.4 ) Pub Date : 2023-11-27 , DOI: 10.1002/zaac.202300195
Marion Graf 1 , Jasmine Ochs 2 , Peter Mayer 1 , Nils Metzler‐Nolte 2 , Hans‐Christian Böttcher 1
Affiliation  

The synthesis and characterization of three compounds [Rh(η5-C5Me5)Cl(N^N)]PF6 (N^N=4,4’-disubstituted-2,2’-bipyridines, 1–3) are described. The cationic complexes contain the bidentate ligands N^N=4,4'-di-tert-butyl-2,2'-bipyridine (1), N^N=4,4'-dinonyl-2,2'-bipyridine (2) and N^N=4,4'-diamino-2,2'-bipyridine (3). The complex salts were obtained by the bridge-splitting reaction from the precursor [{Rh(η5-C5Me5)(μ-Cl)Cl}2] and subsequent salt metathesis affording their corresponding hexafluorido phosphate salts. All compounds were characterized by elemental analysis and spectroscopic means. Additionally, the molecular structure of compound 3 in the solid was determined by a single-crystal X-ray diffraction study. The cytotoxicity of all three compounds was examined by MTT assay against two cancer cell lines – HT-29 (colon adenocarcinoma) and MCF-7 (human breast adenocarcinoma) - and normal human fibroblast cells (GM5657T). Compound 1 has moderate cytotoxicity against both cell lines, while compound 2 is seven to nine times more cytotoxic than cisplatin against MCF-7 and HT-29, respectively. In contrast to cisplatin, both compounds are more active against cancer cells than fibroblasts, thus showing some cancer selectivity.

中文翻译:

一些含有4,4'-二取代-2,2'-联吡啶配体的半夹心铑(III)配合物的细胞毒活性

三种化合物[Rh(η 5 -C 5 Me 5 )Cl(N^N)]PF 6 (N^N=4,4'-二取代-2,2'-联吡啶, 1–3 )的合成与表征被描述。阳离子配合物含有二齿配体 N^N=4,4'-二叔丁基-2,2'-联吡啶 ( 1 )、N^N=4,4'-二壬基-2,2'-联吡啶 ( 2 ) 和 N^N=4,4'-二氨基-2,2'-联吡啶 ( 3 )。通过前体[{Rh(η 5 -C 5 Me 5 )(μ-Cl)Cl} 2 ]的桥断裂反应和随后的盐复分解反应获得其相应的六氟磷酸盐,从而获得复合盐。所有化合物均通过元素分析和光谱手段进行表征。此外,通过单晶 X 射线衍射研究确定了固体中化合物3的分子结构。通过 MTT 测定检测所有三种化合物对两种癌细胞系——HT-29(结肠腺癌)和 MCF-7(人乳腺癌)以及正常人成纤维细胞(GM5657T)的细胞毒性。化合物1对两种细胞系均具有中等细胞毒性,而化合物2对 MCF-7 和 HT-29 的细胞毒性分别是顺铂的 7 至 9 倍。与顺铂相比,这两种化合物对癌细胞的活性比对成纤维细胞的活性更强,因此表现出一定的癌症选择性。
更新日期:2023-11-27
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