Yan Yaw Kai, Melchart Michael, Habtemariam Abraha, Sadler Peter J
School of Chemistry, University of Edinburgh, UK.
Chem Commun (Camb). 2005 Oct 14(38):4764-76. doi: 10.1039/b508531b. Epub 2005 Aug 26.
Our work has shown that certain ruthenium(II) arene complexes exhibit promising anticancer activity in vitro and in vivo. The complexes are stable and water-soluble, and their frameworks provide considerable scope for optimising the design, both in terms of their biological activity and for minimising side-effects by variations in the arene and the other coordinated ligands. Initial studies on amino acids and nucleotides suggest that kinetic and thermodynamic control over a wide spectrum of reactions of Ru(II) arene complexes with biomolecules can be achieved. These Ru(II) arene complexes appear to have an altered profile of biological activity in comparison with metal-based anticancer complexes currently in clinical use or on clinical trial.
我们的研究表明,某些钌(II)芳烃配合物在体外和体内均表现出有前景的抗癌活性。这些配合物稳定且水溶性良好,其结构在优化设计方面提供了相当大的空间,无论是在生物活性方面,还是通过芳烃和其他配位配体的变化来最小化副作用方面。对氨基酸和核苷酸的初步研究表明,钌(II)芳烃配合物与生物分子的广泛反应可实现动力学和热力学控制。与目前正在临床使用或处于临床试验阶段的金属基抗癌配合物相比,这些钌(II)芳烃配合物似乎具有不同的生物活性特征。