The physical and biological properties have been determined for three Pt(IV) complexes with transamine ligands: trans,trans,trans-[PtCl2(OH)2(dimethylamine)(isopropylamine)] (1IV), trans,trans,trans-[PtCl2(OH)2(dimethylamine)(methylamine)] (2IV) and trans,trans,trans-[PtCl2(OH)2(isopropylamine)(methylamine)] (3IV). The crystal structures of 2IV and 3IV reveal substantial strain resulting from repulsion between the amine ligands and the chlorido and hydroxido ligands. All three complexes have reduction potentials in the range −666 to −770 mV, values usually associated with high resistance to reduction and low cytotoxicity. However, the complexes all demonstrate surprisingly high cytotoxicity with values and trends that closely follow those seen for the Pt(II) congeners of these complexes. These results are consistent with more rapid reduction of the Pt(IV) complexes than would be expected based on the reduction potentials, perhaps associated with the trans arrangement of the chlorido ligands.
对于三种含有反式胺
配体的Pt(IV)配合物的物理和
生物学性质已经确定:反式,反式,反式-[PtCl2(OH)2(
二甲基胺)(
异丙基胺)] (1IV)、反式,反式,反式-[PtCl2(OH)2(
二甲基胺)(甲基胺)] (2IV) 和 反式,反式,反式-[PtCl2(OH)2(
异丙基胺)(甲基胺)] (3IV)。2IV和3IV的晶体结构揭示了由于胺
配体与
氯离子和羟基
配体之间的排斥而产生的显著应变。所有三种配合物的还原电位在−666至−770 mV范围内,这些值通常与高抗还原性和低细胞毒性相关。然而,这些配合物却出乎意料地表现出高细胞毒性,其值和趋势与这些配合物的Pt(II)类似物所见的情况紧密相符。这些结果与Pt(IV)配合物的还原速度比基于还原电位所预期的更快一致,可能是由于
氯离子配体的反式排列所致。