Department of Chemistry, University of Warwick, Coventry, CV4 7AL, UK.
Laboratory of Molecular Biology, Center for Cancer Research, NCI, Building 37, Room 5011, Bethesda, MD, 20892-4264, USA.
Angew Chem Int Ed Engl. 2016 Jul 25;55(31):8909-12. doi: 10.1002/anie.201602995. Epub 2016 May 30.
Dinuclear trihydroxido-bridged osmium-arene complexes are inert and biologically inactive, but we show here that linking dihydroxido-bridged Os(II) -arene fragments by a bridging di-imine to form a metallacycle framework results in strong antiproliferative activity towards cancer cells and distinctive knotting of DNA. The shortened spacer length reduces biological activity and stability in solution towards decomposition to biologically inactive dimers. Significant differences in behavior toward plasmid DNA condensation are correlated with biological activity.
双核三羟基桥联锇-芳基配合物是惰性的和无生物活性的，但我们在这里表明，通过桥连二亚胺将二羟基桥联的 Os(II)-芳基片段连接形成金属环框架，导致对癌细胞具有强烈的抗增殖活性，并导致 DNA 独特的打结。较短的间隔物长度会降低溶液中对分解为无生物活性二聚体的生物活性和稳定性。对质粒 DNA 缩合的行为差异与生物活性相关。
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