THE CRYSTAL-STRUCTURES AND ABSOLUTE-CONFIGURATIONS OF THE ANTI-TUMOR COMPLEXES PT(OXALATO)(1R,2R-CYCLOHEXANEDIAMINE) AND PT(MALONATO)(1R,2R-CYCLOHEXANEDIAMINE)

THE CRYSTAL-STRUCTURES AND ABSOLUTE-CONFIGURATIONS OF THE ANTI-TUMOR COMPLEXES PT(OXALATO)(1R,2R-CYCLOHEXANEDIAMINE) AND PT(MALONATO)(1R,2R-CYCLOHEXANEDIAMINE)
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DOI:
10.1016/s0020-1693(00)80051-1
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发表时间:
1984-01-01
期刊:
INORGANICA CHIMICA ACTA-BIOINORGANIC CHEMISTRY
影响因子:
--
通讯作者:
KIDANI, Y
KIDANI, Y
中科院分区:
其他
文献类型:
--
作者:
BRUCK, MA;BAU, R;KIDANI, Y

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用X射线反常散射技术测定了抗肿瘤配合物[Pt(丙二酸根)(trans-l-dach)]和[Pt(丙二酸根)(trans-l-dach)](trans-l-dach = 1 R,2 R-环己二胺)的绝对构型。这些配合物是特别令人感兴趣的,因为它们显示出比具有其它1,2-环己烷二胺(dach)配体的相应Pt配合物,即具有trans-d-dach(1 S,2S-dach)或cis-dach(1 R,2S-dach)的那些配合物更高的抗肿瘤活性。发现双羧酸根和丙二酸根配体以螯合方式通过来自两个羧酸根基团中的每一个的一个氧原子与Pt原子结合。晶体学细节:Pt(Al_2O_3)(trans-l-dach):空间群P21(单斜晶系); a = 11.230(11)nm,B = 9.914(5)nm,c = 4.716(3)nm,β = 90.86(6)°; R = 4.0%(1256次反射)。Pt(丙二酸根)(trans-l-dach):空间群P21(单斜晶系); a = 11.568(5)nm,B = 10.007(5)nm,c = 5.187(3)nm,β = 99.16(4)°; R = 4.8%(1675次反射)。
The absolute configurations of the anti-tumor complexes [Pt(oxalato)(trans-l-dach)] and [Pt(malonato) (trans-l-dach)] (trans-l-dach = 1R,2R-cyclohexanediamine) have been determined by X-ray anomalous scattering techniques. These complexes are particularly interesting because they show higher anti-tumor activity than the corresponding Pt complexes with other 1,2-cyclohexanediamine(dach) ligands, namely those with trans-d-dach (1S,2S-dach) or cis-dach (1R,2S-dach). The oxalato and malonato ligands are found to bind to the Pt atom in a chelating fashion, through one oxygen atom from each of the two carboxylate groups. Crystallographic details: Pt(oxalato)(trans-l-dach): space group P21(monoclinic); a = 11.230(11) Å, b = 9.914(5) Å, c = 4.716(3) Å, β = 90.86(6)°; R = 4.0% for 1256 reflections. Pt(malonato)(trans-l-dach): space group P21(monoclinic); a = 11.568(5) Å, b = 10.007(5) Å, c = 5.187(3) Å, β = 99.16(4)°; R = 4.8% for 1675 reflections.