Departamento de Química Inorgánica (Módulo 07), Facultad de Ciencias, Universidad Autónoma de Madrid, Madrid, Spain.
J Inorg Biochem. 2011 Dec;105(12):1613-22. doi: 10.1016/j.jinorgbio.2011.08.014. Epub 2011 Aug 28.
Treatment of (4)N-monosubstituted bis(thiosemicarbazone) ligands of 3,5-diacetyl-1,2,4-triazol series with lithium tetrachloridopalladate gave the dinuclear complexes of general formula Pd(μ-H(3)L(1-5)), but using dichloridobistriphenylphosphinepalladium(II) salt, the first mononuclear bis(thiosemicarbazone)-palladium-triphenylphosphine complexes of the 3,5-diacetyl-1,2,4-triazol series, [Pd(H(3)L(1-5))PPh(3)], have been obtained. All the compounds have been characterized by elemental analysis and by IR and NMR spectroscopy, and the crystal and molecular structures of dinuclear complexes Pd(μ-H(3)L(3)) and Pd(μ-H(3)L(5)) as well as mononuclear complexes [Pd(H(3)L(1))PPh(3)], [Pd(H(3)L(2))PPh(3)], [Pd(H(3)L(3))PPh(3)] and [Pd(H(3)L(4))PPh(3)] have been determined by X-ray crystallography. The new compounds synthesized have been evaluated for antiproliferative activity in vitro against NCI-H460, A2780 and A2780cisR human cancer cell lines. Subsequent toxicity study, on normal renal LLC-PK1 cells, shows that all compounds investigated exhibit very low toxicity on kidney cells with respect to cisplatin.
用四氯钯酸钠与 3,5-二乙酰基-1,2,4-三唑系列的 4N-单取代双（硫代缩氨基脲）配体反应得到双核配合物Pd(μ-H(3)L(1-5))，但使用二氯二（三苯基膦）钯(II)盐，则得到了 3,5-二乙酰基-1,2,4-三唑系列的第一个单核双（硫代缩氨基脲）-钯-三苯基膦配合物[Pd(H(3)L(1-5))PPh(3)]。所有化合物均通过元素分析和 IR、NMR 光谱进行了表征，并通过 X 射线晶体学确定了双核配合物Pd(μ-H(3)L(3))和Pd(μ-H(3)L(5))以及单核配合物[Pd(H(3)L(1))PPh(3)]、[Pd(H(3)L(2))PPh(3)]、[Pd(H(3)L(3))PPh(3)]和[Pd(H(3)L(4))PPh(3)]的晶体和分子结构。所合成的新化合物在体外针对 NCI-H460、A2780 和 A2780cisR 人癌细胞系进行了抗增殖活性评估。随后对正常肾 LLC-PK1 细胞进行的毒性研究表明，与顺铂相比，所有研究的化合物对肾细胞的毒性都非常低。
