Departamento de Química Orgánica e Inorgánica, Instituto de Química Organometálica Enrique Moles (Unidad Asociada al C.S.I.C.). Universidad de Oviedo, 33006, Oviedo, Spain.
Dalton Trans. 2010 Nov 14;39(42):10186-96. doi: 10.1039/c0dt00206b. Epub 2010 Sep 30.
The synthesis and full characterization of new half-sandwich ruthenium(II) complexes containing κ(3)(N,N,N)-hydridotris(pyrazolyl)borate (κ(3)(N,N,N)-Tp) and the water-soluble phosphanes 1,3,5-triaza-7-phosphatricyclo[3.3.1.1(3,7)]decane (PTA) and 1-methyl-3,5-diaza-1-azonia-7-phosphatricyclo[3.3.1.1(3,7)]decane (1-CH(3)-PTA) has been explored. Single crystal X-ray diffraction analysis for complex [RuCl{κ(3)(N,N,N)-Tp}(PMe(2)Ph)(1-CH(3)-PTA)][CF(3)SO(3)]·2NCMe is also reported. DNA binding properties of the ruthenium complexes have been evaluated by mobility shift assay and MALDI-TOF mass spectrometry. The in vitro antitumor activity of these compounds was assessed by examining their ability to inhibit cell proliferation in a number of human cancer cell lines (NCI-H460, SF-268, MCF-7) and non-tumor human umbilical vein endothelial cells (HUVEC). Some of these new compounds show promising cytotoxic activity with IC(50) values in the low micromolar range, and display differential effects on cancer and normal cell growth.
新的半夹心型钌（II）配合物的合成及全谱特性研究，这些配合物包含κ(3)(N,N,N)-氢代三（吡唑基）硼酸盐（κ(3)(N,N,N)-Tp）和水溶性膦配体 1,3,5-三氮杂-7-磷杂三环[3.3.1.1(3,7)]癸烷（PTA）和 1-甲基-3,5-二氮杂-1-氮杂-7-磷杂三环[3.3.1.1(3,7)]癸烷（1-CH(3)-PTA）。并对配合物[RuCl{κ(3)(N,N,N)-Tp}(PMe(2)Ph)(1-CH(3)-PTA)][CF(3)SO(3)]·2NCMe 的单晶 X 射线衍射分析进行了报道。通过迁移率变动分析和 MALDI-TOF 质谱法评估了这些钌配合物的 DNA 结合特性。通过检测它们在多种人类癌细胞系（NCI-H460、SF-268、MCF-7）和非肿瘤人类脐静脉内皮细胞（HUVEC）中抑制细胞增殖的能力，评估了这些化合物的体外抗肿瘤活性。一些新的化合物表现出有希望的细胞毒性活性，IC(50)值在低微摩尔范围内，并对癌症和正常细胞生长显示出不同的影响。
