Khokhar A R, Xu Q, Siddik Z H
Department of Clinical Investigation, University of Texas M.D. Anderson Cancer Center, Houston.
J Inorg Biochem. 1994 Mar;53(4):295-301. doi: 10.1016/0162-0134(94)85116-6.
A series of novel water-soluble amine platinum (II) tellurate complexes of the type (A)Pt(II) [TeO2(OH)4], where A = 1,2-diaminocyclohexane (DACH), 1,1-bis(aminomethyl)cyclohexane (AMCH), ethylenediamine (en), or cyclopentylamine (cpa), were prepared either by the reaction of amineplatinum (II) sulfate with barium tellurate or by a direct reaction of (A)Pt(OH)2 with telluric acid. Oxidation of the amine platinum(II) tellurate produced amine platinum(IV) tellurate (A)Pt(IV)trans(Z) [TeO2(OH)4] complexes, where Z = OH or Cl, following oxidation with hydrogen peroxide or with chlorine gas, respectively. Complexes were characterized by elemental analysis, and IR and 195Pt NMR spectroscopy. Against i.p. murine leukemia cells in vivo, some of the complexes displayed good antitumor activity when administered intraperitoneally (i.p.) on days 1, 5, and 9 at their optimal doses. Pt(II) complexes containing R,R-DACH, S,S-DACH, R,R-S,S-DACH, or AMCH produced %T/C of 147 to 288 whereas cis-DACH, en, and cpa complexes were inactive. In the Pt(IV) series, the R,R-DACH complex with axial Cl was highly active (%T/C = 371, 40% cures) compared with the complex with axial OH (%T/C = 135).
制备了一系列新型的水溶性胺铂（II）碲酸盐配合物，其通式为（A）Pt（II）[TeO₂(OH)₄]，其中A = 1,2 - 二氨基环己烷（DACH）、1,1 - 双（氨甲基）环己烷（AMCH）、乙二胺（en）或环戊胺（cpa），制备方法要么是胺铂（II）硫酸盐与碲酸钡反应，要么是（A）Pt(OH)₂与碲酸直接反应。胺铂（II）碲酸盐经氧化分别生成胺铂（IV）碲酸盐（A）Pt（IV）trans(Z)[TeO₂(OH)₄]配合物，其中Z = OH或Cl，分别用过氧化氢或氯气氧化。通过元素分析、红外光谱和¹⁹⁵Pt核磁共振光谱对配合物进行了表征。在体内对腹腔注射的小鼠白血病细胞进行实验时，一些配合物在第1、5和9天以最佳剂量腹腔注射给药时显示出良好抗癌活性。含R,R - DACH、S,S - DACH、R,R - S,S - DACH或AMCH的Pt（II）配合物的%T/C为147至288，而顺式 - DACH、en和cpa配合物无活性。在Pt（IV）系列中，与轴向为OH的配合物（%T/C = 135）相比，轴向为Cl 的R,R - DACH配合物具有高活性（%T/C = 371，治愈率40%）。
