Binding site and equilibrium constant of ethylenediamineplatinum(II) or triamineplatinum(II) to thymidine

Kenji Inagaki, Yoshinori Kidani
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引用次数: 4

Abstract

The complex of thymidine with (NH3)3Pt(OH2) or (en)Pt(OH2)2, where en = ethylenediamine, have been prepared in aqueous solution at pH = 7. The isolated complexes, corresponding to the formula [(NH3)3Pt(ThdH−1)]NO3 and (en)Pt(ThdH−1)2 where ThdH−1 = mono anion of thymidine, have been characterized by nmr, ir, and uv spectra. The binding site is the N(3) position of ThdH−1.

The equilibrium constant for (NH3)3Pt(OH2) + ThdH−1 ⇌ (NH3)3Pt(ThdH−1), in which the equilibrium of binding is pH dependent, was estimated from integrated intensity ratio of the proton of position 6 of thymidine, and log K was 10.4 ± 0.1. In the case of (en)Pt(ThdH−1)2, the log K1 for (en)Pt(OH2)2 + ThdH−1 ⇌ (en)Pt(OH2)(ThdH−1) was 10.3 ± 0.1, and the log K2 for (en)Pt(OH2)(ThdH−1) + ThdH−1 ⇌ (en)Pt(ThdH−1)2 was 7.4 ± 0.1.

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乙二胺铂(II)或三胺铂(II)与胸苷的结合位点和平衡常数
在pH = 7的水溶液中制备了胸腺嘧啶与(NH3)3Pt(OH2)或(en)Pt(OH2)2的络合物,其中en =乙二胺。分子式为[(NH3)3Pt(ThdH−1)]NO3和(en)Pt(ThdH−1)2,其中ThdH−1 =胸腺嘧啶的单阴离子,用nmr、ir和uv光谱对其进行了表征。结合位点是ThdH−1的N(3)位。根据胸腺嘧啶第6位质子的积分强度比,估计了(NH3)3Pt(OH2) + ThdH−1 + (NH3)3Pt(ThdH−1)的平衡常数,其结合平衡与pH有关,对数K为10.4±0.1。以(en)Pt(ThdH−1)2为例,(en)Pt(OH2)2 + ThdH−1 + (en)Pt(OH2)(ThdH−1)+ ThdH−1 + (en)Pt(ThdH−1)2的对数K1为10.3±0.1,(en)Pt(OH2)(ThdH−1)+ ThdH−1 + (en)Pt(ThdH−1)2的对数K2为7.4±0.1。
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