Williams John W, Qu Yun, Bulluss Genevieve H, Alvorado Eugenio, Farrell Nicholas P
Department of Chemistry, Virginia Commonwealth University, Richmond, Virginia 23284-2006, USA.
Inorg Chem. 2007 Jul 23;46(15):5820-2. doi: 10.1021/ic700410y. Epub 2007 Jun 26.
The synthesis of bifunctional dinuclear platinum complexes, {PtCl(dach)}(2)-mu-YCl(n) (1-3; Y = H(2)N(CH(2))(3)NH(2)(CH(2))(4)NH(2), H(2)N(CH(2))(6)NH(2)(CH(2))(6)NH(2), and H(2)N(CH(2))(6)NH(2)(CH(2))(2)NH(2)(CH(2))(6)NH(2), respectively; Figure 1) is reported. There was no labilization of the polyamine linker groups of the cis-1,2-diaminocyclohexane complexes in the presence of sulfur-containing species at physiological pH, in contrast to previous studies preformed on trans complexes. Metabolism reactions are somewhat dependent on the nature of the polyamine: at physiological pH, the spermidine complex 1 forms an inert (tetraamine)platinum species in which one platinum is chelated by a central and terminal amino group. The stability of cis-geometry complexes may make them viable second-generation polynuclear platinum clinical candidates.
报道了双功能双核铂配合物{PtCl(dach)}(2)-μ-YCl(n)（1 - 3；Y分别为H(2)N(CH(2))(3)NH(2)(CH(2))(4)NH(2)、H(2)N(CH(2))(6)NH(2)(CH(2))(6)NH(2)和H(2)N(CH(2))(6)NH(2)(CH(2))(2)NH(2)(CH(2))(6)NH(2)；图1）的合成。与之前对反式配合物进行的研究相反，在生理pH值下，含硫物质存在时，顺式-1,2-二氨基环己烷配合物的多胺连接基团没有发生不稳定化。代谢反应在某种程度上取决于多胺的性质：在生理pH值下，亚精胺配合物1形成一种惰性的（四胺）铂物种，其中一个铂被一个中心氨基和一个末端氨基螯合。顺式几何构型配合物的稳定性可能使其成为可行的第二代多核铂临床候选物。
