含钯环的1,4-苯二氮䓬的合成及其体外抗癌活性和组织蛋白酶B活性
Synthesis of a 1,4-benzodiazepine containing palladacycle with in vitro anticancer and cathepsin B activity.
作者信息
Spencer John, Rathnam Rajendra P, Motukuri Mahesh, Kotha Arun K, Richardson Simon C W, Hazrati Ali, Hartley John A, Male Louise, Hursthouse Michael B
机构信息
School of Science, University of Greenwich at Medway, Chatham Maritime, UK.
出版信息
Dalton Trans. 2009 Jun 14(22):4299-303. doi: 10.1039/b819061e. Epub 2009 Jan 29.
The reaction of the five-membered C,N-palladacycle (L)PdCl, where LH = 1-methyl-5-phenyl-1H-1,4-benzodiazepin-2(3H)-one, with 1,2-ethanebis(diphenylphosphine), dppe, leads to the formation of the bridged palladacycle. [Pd(2)L(2)(mu-dppe)Cl(2)] 3, which was characterised in solution by (1)H and (31)P NMR spectroscopy and in the solid state by X-ray crystallography. Complex 3 was tested in vitro against a number of cell lines. For example, it inhibited K562 leukaemia cells with an IC(50) value of 4.3 microM (1 h exposure) and displayed cathepsin B inhibitory action with an IC(50) value of 3 microM.
五元C，N-钯环化合物(L)PdCl（其中LH = 1-甲基-5-苯基-1H-1,4-苯并二氮杂卓-2(3H)-酮）与1,2-乙二双（二苯基膦）（dppe）反应，生成桥连钯环化合物[Pd(2)L(2)(μ-dppe)Cl(2)] 3，该化合物通过(1)H和(31)P NMR光谱在溶液中进行了表征，并通过X射线晶体学在固态下进行了表征。化合物3在体外针对多种细胞系进行了测试。例如，它对K562白血病细胞具有抑制作用，IC(50)值为4.3 microM（暴露1小时），并且对组织蛋白酶B具有抑制作用，IC(50)值为3 microM。
Zotero 插件