Faculty of Chemistry, Nicolaus Copernicus University, Gagarina 7, 87-100 Toruń, Poland.
Dalton Trans. 2013 May 7;42(17):6219-26. doi: 10.1039/c2dt32216a. Epub 2013 Jan 18.
Two ruthenium(III) complexes composed of 5,7-ditertbutyl-1,2,4-triazolo[1,5-a]pyrimidine (dbtp) ligands were prepared and structurally characterized by X-ray crystallography, IR, UV-Vis, EPR spectroscopies and cyclic voltammetry (CV). The crystal structures of trans-[RuCl(3)(H(2)O)(dbtp)(2)] 1 and mer-[RuCl(3)(dbtp)(3)]·0.815OCMe(2) 2 showed slightly distorted octahedral geometries with two 1 or three 2 monodentate dbtp ligands bound in a head-to-head orientation. In both complexes, the heterocyclic dbtp ligands were bound to the ruthenium(III) ion through the N3 nitrogen atom. A cytotoxicity assay of both ruthenium(III) compounds against two human cell lines (A549 - non-small cell lung carcinoma and T47D - breast carcinoma) was performed. The ruthenium(III) complexes showed excellent cytotoxicity with IC(50) values in the range of 0.02-2.4 μM against both cancer cell lines. In addition, the in vitro cytotoxic values of the ruthenium(III) compounds were 35-times for 1 and 172-times for 2 higher against T47D than the clinically used antitumor drug cisplatin.
合成了两个钌(III)配合物，它们由 5,7-二叔丁基-1,2,4-三唑并[1,5-a]嘧啶(dbtp)配体组成，并通过 X 射线晶体学、红外光谱、紫外可见光谱、电子顺磁共振光谱和循环伏安法(CV)进行了结构表征。反式-[RuCl(3)(H(2)O)(dbtp)(2)]1 和内消旋-[RuCl(3)(dbtp)(3)]·0.815OCMe(2)2 的晶体结构显示出略微扭曲的八面体几何形状，其中两个 1 或三个 2 个单齿 dbtp 配体以头对头的方式配位。在这两个配合物中，杂环 dbtp 配体通过 N3 氮原子与钌(III)离子配位。对两种人癌细胞系(A549-非小细胞肺癌和 T47D-乳腺癌)进行了两种钌(III)化合物的细胞毒性测定。这两种钌(III)配合物对两种癌细胞系均表现出优异的细胞毒性，IC(50)值在 0.02-2.4 μM 范围内。此外，1 对 T47D 的体外细胞毒性值比临床使用的抗肿瘤药物顺铂高 35 倍，2 对 T47D 的体外细胞毒性值比顺铂高 172 倍。
