Metal-arene complexes containing bioactive natural-product derived ligands can have new and unusual properties. We report the synthesis, characterization and antiproliferative activity of two new Ru(II) arene complexes with imidazole (dichlorido complex 1) or bipyridyl (chlorido complex 2) ligands conjugated to 18β-glycyrrhetinic acid, an active triterpenoid metabolite of Glycyrrhiza glabra. In general, the conjugated ligands and complexes showed only moderate activity against HeLa (cervical), MCF-7 (breast) and A2780 (ovarian) cancer cells, although the activity of complex 2 in the former two cell lines approached that of the drug cisplatin. Complex 2 (in contrast to complex 1) also exhibited significant activity towards both Gram-positive S. aureus and Gram-negative E. coil bacteria. Complex 2 can induce condensation of DNA and enhances the generation of intracellular reactive oxygen species (ROS). The conjugation of natural products to ligands in organometallic half-sandwich complexes provides a strategy to enhance their biological activities.

含有生物活性天然产物衍生的配体的金属芳烃配合物可以具有新的和异常的特性。我们报告的合成，表征和两个新的Ru（II）的抗增殖活性芳烃与咪唑络合物（dichlorido复杂1）或联吡啶（chlorido复杂2）的配体缀合到18β-甘草次酸，的活性代谢物三萜光果甘草。通常，虽然前两个细胞系中复合物2的活性接近顺铂药物，但缀合的配体和复合物仅对HeLa（宫颈），MCF-7（乳腺癌）和A2780（卵巢）癌细胞具有中等活性。。复合体2（与复合体1相反）对革兰氏阳性S均表现出显着活性。金黄色葡萄球菌和革兰氏阴性ê。盘绕细菌。配合物2可以诱导DNA缩合，并增强细胞内活性氧（ROS）的生成。天然产物与有机金属半三明治复合物中配体的缀合提供了增强其生物活性的策略。