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使用质子核磁共振方法测定了新的抗癌活性配合物cis-[Pt(NH3)2(4-mepy)Cl]+与甲基-谷胱甘肽(GS-Me)的反应及其动力学.结果表明Pt与GS-Me间形成1:1加合物.为了解结合部位,对Pt-GS-Me配合物进行pH滴定,由GS-Me的质子核磁共振谱对pH的依赖关系判断Gs-Me只通过S原子与Pt配位,而氨基和羧基不参与配位反应.由配体吡啶环质子核磁共振随时间的变化,提出了两步反应机制:首先GS-Me通过S原子与Pt配位,然后由于S配位的高度反位效应使反应的NH3活动化.通过1HNMR方法测定了第一步反应的速率常数k=0.017L·mol-1·s-1(pH3.1)和k=0.013L·mol-1·s-1(pH7.2).
The reaction and kinetics of the novel antitumor complex cis- [Pt (NH3) 2 (4-mepy) Cl] + with methyl-glutathione (GS-Me) were determined by proton NMR. The results show that Pt and GS-Me form a 1: 1 adduct. In order to understand the binding sites, pH-titration of Pt-GS-Me complexes was carried out. The dependence of pH on the proton nuclear magnetic resonance spectrum of GS-Me determined that Gs-Me only coordinated to Pt through S atoms, while the amino and carboxyl groups did not participate Coordination reaction. The two-step reaction mechanism is proposed by the change of the proton nuclear magnetic resonance of the pyridine ring with time. First, GS-Me coordinates with Pt through the S atom, and then NH3 is activated due to the highly anti-site effect of S coordination. The rate constant k = 0.017L · mol-1 · s-1 (pH3.1) and k = 0.013L · mol-1 · s-1 (pH7.2) of the first reaction were determined by 1HNMR method.