Novel coordinatively saturated platinum(II) compounds bearing C-linked carbohydrates were synthesized and characterized. The complexes exhibit bipyramidal trigonal geometry with a bidentate nitrogen ligand and ethylene in the equatorial plane. The axial positions are occupied by a halide ligand X and a D-galactose or D-glucose derivative, linked either via C1 or C6. The compounds were designed for evaluation of the biological activity because they combine the steady coordinative saturation, the beneficial action of the modular sugar moiety and the organometallic nature of the Pt-sugar linkage, which is expected to be stable in the biological media, until the target is reached. The newly synthesized molecules were stable in mixed DMSO/aqueous solvents, able to bind DNA in vitro and exhibited a selective cytotoxic activity on cancer cells through apoptosis activation.

中文翻译：

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铂基药物中的C-糖基化：提高细胞毒性和选择性的可行策略†

合成和表征新型的配位饱和的带有C键联的碳水化合物的铂（II）化合物。所述配合物表现出具有在赤道平面中的双齿氮配体和乙烯的双锥体三角几何形状。轴向位置被卤化物配体X和D-半乳糖或D-葡萄糖衍生物占据，它们通过以下方式连接C1或C6。这些化合物设计用于评估生物活性，因为它们结合了稳定的配位饱和度，模块糖部分的有益作用以及Pt糖键的有机金属性质（预计在生物介质中稳定），直到达到目标。新合成的分子在混合的DMSO /水性溶剂中稳定，能够在体外结合DNA ，并通过凋亡激活对癌细胞表现出选择性的细胞毒活性。