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Os2–Os4 Switch Controls DNA Knotting and Anticancer Activity |
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| Authors: | Dr Ying Fu Dr María J Romero Dr Luca Salassa Dr Xi Cheng Dr Abraha Habtemariam Dr Guy J Clarkson Dr Ivan Prokes Prof Alison Rodger Prof Giovanni Costantini Prof Peter J Sadler |
| Institution: | 1. Department of Chemistry, University of Warwick, Coventry, UK;2. Laboratory of Molecular Biology, Center for Cancer Research, NCI, Bethesda, MD, USA;3. Departamento de Química Inorgánica, Facultade de Química, Universidade de Santiago de Compostela, Santiago de Compostela, Spain;4. CIC biomaGUNE, Donostia-San Sebastián, Spain |
| Abstract: | Dinuclear trihydroxido‐bridged osmium–arene complexes are inert and biologically inactive, but we show here that linking dihydroxido‐bridged OsII–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. |
| Keywords: | cancer DNA organometallic osmium supramolecular |