Non-coordination planer cis-and trans-configuration of cis-[Pt(II)(mixed-NH3/RNH2)(3-OH-cyclobutane-1,1-dicarboxylate)]: separation, characterization, and anticancer activity

Non-coordination planer cis-and trans-configuration of cis-[Pt(II)(mixed-NH3/RNH2)(3-OH-cyclobutane-1,1-dicarboxylate)]: separation, characterization, and anticancer activity
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顺式-[Pt(II)(mixed-NH3/RNH2)(3-OH-cyclobutane-1,1-dicarboxylate)]的非配位平面顺式和反式构型:分离、表征和抗癌活性

DOI:
10.1007/s11164-018-3503-0
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发表时间:
2018-06
影响因子:
3.3
通讯作者:
Weiping Liu
Weiping Liu
中科院分区:
化学3区
文献类型:
--
作者:
Jing Jiang;Jie Qiu;Liguang Lou;Anli Gao;Shuqian Hou;Weiping Liu

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分离了cis-[Pt(II)(mixed-NH3/RNH2)(3-OH-cyclobutane-1,1-dicarboxylate)]的两个异构体(R- = 环戊基、环己基),并对其进行了结构表征和抗癌活性测试。X-射线结构分析表明,该异构体来源于环丁烷环上羟基相对于配位NH3的两个相反的空间取向,导致顺式和反式构型。这两个异构体具有大致相同的抗癌活性,可能是由于羟基和铂(II)配位平面之间的距离较长。因此,在药物开发过程中不建议分离这种异构体。
Two isomers of cis-[Pt(II)(mixed-NH3/RNH2)(3-OH-cyclobutane-1,1-dicarboxylate)] (R = cycopentyl, cyclohexyl) were separated, structurally characterized and tested for their anticancer activity. X-ray structural analysis revealed that this isomerism originates from two opposite spatial orientations of the hydroxyl group on the cyclobutane ring in relation to the coordinated NH3, resulting in cis- and trans-configurations. The two isomers have approximately equal anticancer activity, probably due to a relatively long distance between the hydroxyl group and the Pt(II) coordination plane. Therefore, the separation of such isomers is not recommended during drug development.
DOI: 10.1039/c0dt00292e
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