Synthesis of a 1,4-benzodiazepine containing palladacycle with in vitro anticancer and cathepsin B activity.
Synthesis of a 1,4-benzodiazepine containing palladacycle with in vitro anticancer and cathepsin B activity.
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DOI：
10.1039/b819061e
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发表时间：
2009-05
影响因子：
4
通讯作者：
J. Spencer;Rajendra P. Rathnam;Mahesh Motukuri;A. Kotha;S. Richardson;A. Hazrati;J. Hartley;L. Male;M. Hursthouse
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文献类型：
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作者：
J. Spencer;Rajendra P. Rathnam;Mahesh Motukuri;A. Kotha;S. Richardson;A. Hazrati;J. Hartley;L. Male;M. Hursthouse
五元C，N-钯配体[（L）PdCl]（2）（LH = 1-甲基-5-苯基-1H-1，4-苯并二氮杂卓-2（3 H）-酮）与1，2-乙烷双（二苯基膦）dppe反应，生成桥联钯配体。[Pd（2）L（2）（mu-dppe）Cl（2）] 3，其在溶液中通过（1）H和（31）P NMR光谱表征，在固态下通过X射线晶体学表征。在体外针对许多细胞系测试复合物3。例如，它抑制K562白血病细胞的IC（50）值为4.3 μ M（1小时暴露），并显示组织蛋白酶B抑制作用的IC（50）值为3 μ M。
The reaction of the five-membered C,N-palladacycle [(L)PdCl](2), 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.