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氨基取代氧化膦的铂(II)、铂(IV)和钯(II)配合物:合成、表征及抗肿瘤活性

Platinum(II), platinum(IV), and palladium (II) complexes of amino substituted phosphine oxides: synthesis, characterization, and antitumor activity.

作者信息

Dodoff N, Varbanov S, Borisov G, Spassovska N

机构信息

Institute of Molecular Biology, Bulgarian Academy of Sciences, Sofia.

出版信息

J Inorg Biochem. 1990 Jul;39(3):201-8. doi: 10.1016/0162-0134(90)84003-8.

Abstract

The complexes [Pt(dapo)2Cl2], [PtNH3(dapo)Cl2], [Pt(py)(dapo)Cl2], [Pt(mbpo)Cl2].H2O, [Pt(mbpo)(OH)2Cl2].H2O, [Pd(dapo)2Cl2], and [Pd(mbpo)Cl2], where dapo is dimethyl aminomethylphosphine oxide and mbpo is methyl bis(aminomethyl)phosphite oxide have been synthesized and characterized by elemental analyses, electric conductivity, infrared, 1H NMR and electronic spectra. The ligands are found to be coordinated only via the amino groups. The complexes are of cis-square planar configuration with the exception of [Pt(mbpo)(OH)2Cl2].H2O which is pseudo-octahedral. An in vivo antitumor screening of the complexes against Leukemia L1210 was performed. A considerable activity (T/C = 233%) was observed for [PtNH3(dapo)Cl2]. The activity of the remaining complexes was below the accepted criterion.

摘要

已合成了配合物[Pt(dapo)₂Cl₂]、[PtNH₃(dapo)Cl₂]、[Pt(py)(dapo)Cl₂]、[Pt(mbpo)Cl₂]·H₂O、[Pt(mbpo)(OH)₂Cl₂]·H₂O、[Pd(dapo)₂Cl₂]和[Pd(mbpo)Cl₂],其中dapo为二甲基氨甲基氧化膦,mbpo为甲基双(氨甲基)亚磷酸氧化膦,并通过元素分析、电导率、红外光谱、¹H NMR和电子光谱对其进行了表征。发现配体仅通过氨基配位。除了[Pt(mbpo)(OH)₂Cl₂]·H₂O为假八面体构型外,这些配合物均为顺式平面正方形构型。对这些配合物进行了针对白血病L1210的体内抗肿瘤筛选。观察到[PtNH₃(dapo)Cl₂]具有相当的活性(T/C = 233%)。其余配合物的活性低于公认标准。

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