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Syntheses and Cytotoxicity of Pt(II) Complexes with Acyclovir

机译:阿昔洛韦与Pt(II)配合物的合成及细胞毒性

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Acyclovir is an antiviral drug which acts against the viruses,including Herpes simplex 1 and 2 and Varicella-zoster.The novel cis-[PtI_2(3-Hmpy)_2](3-Hmpy = 3-hydroxymethylpyridine)(2) and the water-soluble cationic Pt(II) complexes with acyclovir (acv,(9-[(2-hydroxyetoxy)methyl]guanine)),cis-[Pt(acv-N_7)_2(NH_3)_2]Cl_2 centre dot 2H_2O (1) and cis-[Pt(acv-N_7)_2(3-Hmpy)_2](NO_3)_2 (3),have been prepared and characterized by multinuclear NMR spectroscopy.The results of cytotoxicity assay of 1,3 and cis-[PtCl_2(NH_3)_2] (cisplatin,cDDP) performed in malignant melanoma B16 cells in vitro provide evidence that complex 1 and 3 are less cytotoxic compared to cisplatin.In vivo experiments performed on the same malignant melanoma B16 cells,grown as subcutaneous tumours,demonstrated that antitumour effectiveness of 1 was comparable to that of cisplatin.
机译:阿昔洛韦是一种抗病毒药,可对抗包括单纯疱疹1和2和水痘带状疱疹在内的病毒起作用。新型的顺式[[PtI_2(3-Hmpy)_2](3-Hmpy = 3-羟甲基吡啶)(2)和水环糊精与阿昔洛韦(acv,(9-[(2-羟基羟氧基)甲基]鸟嘌呤)),顺式[Pt(acv-N_7)_2(NH_3)_2] Cl_2中心点2H_2O的阳离子Pt(II)配合物(1)制备了顺式[Pt(acv-N_7)_2(3-Hmpy)_2](NO_3)_2(3)并对其进行了表征。1,3和顺式[PtCl_2]的细胞毒性测定结果(NH_3)_2](cisplatin,cDDP)在体外在恶性黑色素瘤B16细胞中提供的证据表明,与顺铂相比,复合物1和3的细胞毒性更小。 1的抗肿瘤效力与顺铂相当。

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