首页> 美国卫生研究院文献>Metal-Based Drugs >Ternary Complexes of cis-(NH3)2PtCl2 (cis-DDP) With Guanosine (guo) Cytidine (cyd) and the Aminoacids Glycine (gly) L-Alanine (ala) L-2-Aminobutyric Acid (2-aba) L-Norvaline (nval) and L-Norleucine (nleu)
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Ternary Complexes of cis-(NH3)2PtCl2 (cis-DDP) With Guanosine (guo) Cytidine (cyd) and the Aminoacids Glycine (gly) L-Alanine (ala) L-2-Aminobutyric Acid (2-aba) L-Norvaline (nval) and L-Norleucine (nleu)

机译:顺式-(NH3)2PtCl2(顺式-DDP)与鸟苷(guo)胞苷(cyd)和氨基酸甘氨酸(gly)L-丙氨酸(ala)L-2-氨基丁酸(2-aba)的三元复合物L-正缬氨酸(nval)和L-正亮氨酸(nleu)

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摘要

The ternary complexes of formulae cis-[(NH3)2Pt(nucl)(amac)]NO3, where nucl = guo and cyd (guanosine and cytidine) and amac = the deprotonated aminoacids glycine (gly), L-alanine (ala), L-2-aminobutyric acid (2-aba), L-norvaline (nval) and L-norleucine (nleu), were prepared from the reactions of the binary chelated ones cis-[(NH3)2Pt(nucl)(amac)]NO3 with the nucleosides.They were characterized by 1H, 13C and 195Pt NMR and IR spectra, together with elemental analysis and conductivity measurements. The aminoacids coordinate with Pt(II) in the ternary complexes with their terminal -NH2 groups, guo through N7 and cyd through N3. Ligand-ligand hydrophobic interactions were also observed in the ternary complexes and were stronger with longer aliphatic chains of the aminoacids. The 3E sugar conformation increased by 5-7% in the ternary systems, as compared to the free nucleosides, while the percentage of the gg conformation remained almost constant and the one of the anti conformation of the sugar increased also slightly. Finally, the h conformer around the Cα-Cβ bonds of the aminoacids reached a maximum in the binary systems and decreased again considerably in the ternary ones.
机译:式cis-[(NH3)2Pt(nucl)(amac)] NO3的三元配合物,其中nucl = guo和cyd(鸟苷和胞苷),而amac =去质子化氨基酸甘氨酸(gly),L-丙氨酸(ala), L-2-氨基丁酸(2-aba),L-正缬氨酸(nval)和L-正亮氨酸(nleu)是由二元螯合的顺式[[(NH3)2Pt(nucl)(amac)]反应制得的NO3带有核苷。它们的特征在于 1 H, 13 C和 195 Pt NMR和IR光谱,以及元素分析和电导率测量。氨基酸在其端基为-NH2的三元配合物中与Pt(II)配位,即guo至N7和cyd至N3。在三元络合物中也观察到配体-配体疏水相互作用,并且在氨基酸的更长的脂族链上更强。与游离核苷相比,三元系统中的 3 E糖构象增加了5-7%,而gg构象的百分比几乎保持恒定,并且是糖的反构象之一也略有增加。最后,在氨基酸的Cα-Cβ键周围的h构象子在二元系统中达到最大值,而在三元系统中又大大降低。

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