Institute of Organic Chemistry (IOC) , Karlsruhe Institute of Technology (KIT) , Fritz-Haber-Weg 6 , 76131 Karlsruhe , Germany.
Institute of Functional Interfaces (IFG) , Karlsruhe Institute of Technology (KIT) , Hermann von Helmholtz Platz 1 , 76344 Eggenstein-Leopoldshafen , Germany.
Inorg Chem. 2019 Dec 2;58(23):15917-15926. doi: 10.1021/acs.inorgchem.9b02402. Epub 2019 Nov 12.
A range of novel cyclometalated ruthenium(II) and iridium(III) complexes with a steroidal backbone based on androsterone were synthesized and characterized by NMR spectroscopy and X-ray crystallography. Their cytotoxic properties in RT112 and RT112 cP (cisplatin-resistant) cell lines as well as in MCF7 and somatic fibroblasts were compared with those of the corresponding nonsteroidal complexes and the noncyclometalated pyridyl complexes as well as with cisplatin as reference. All steroidal complexes were more active in RT112 cP cells than cisplatin, whereby the cyclometalated pyridinylphenyl complexes based on showed high cytotoxicity while maintaining low resistant factors of 0.33 and 0.50.
合成了一系列基于雄甾酮的新型甾体骨架的钉(II)和铱(III)配合物，并通过 NMR 光谱和 X 射线晶体学进行了表征。将它们在 RT112 和 RT112 cP（顺铂耐药）细胞系以及 MCF7 和体成纤维细胞中的细胞毒性与相应的非甾体配合物以及非环金属化的吡啶基配合物以及顺铂进行了比较。所有甾体配合物在 RT112 cP 细胞中的活性均高于顺铂，其中基于的钉的环金属化吡啶基苯基配合物具有很高的细胞毒性，同时保持低耐药因子 0.33 和 0.50。
