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Os2 -Os4 Switch Controls DNA Knotting and Anticancer Activity.
Fu, Ying; Romero, María J; Salassa, Luca; Cheng, Xi; Habtemariam, Abraha; Clarkson, Guy J; Prokes, Ivan; Rodger, Alison; Costantini, Giovanni; Sadler, Peter J.
Afiliación
  • Fu Y; Department of Chemistry, University of Warwick, Coventry, CV4 7AL, UK.
  • Romero MJ; Laboratory of Molecular Biology, Center for Cancer Research, NCI, Building 37, Room 5011, Bethesda, MD, 20892-4264, USA.
  • Salassa L; Department of Chemistry, University of Warwick, Coventry, CV4 7AL, UK.
  • Cheng X; Departamento de Química Inorgánica, Facultade de Química, Universidade de Santiago de Compostela, 15782, Santiago de Compostela, Spain.
  • Habtemariam A; Department of Chemistry, University of Warwick, Coventry, CV4 7AL, UK.
  • Clarkson GJ; CIC biomaGUNE, Paseo de Miramón 182, 20009, Donostia-San Sebastián, Spain.
  • Prokes I; Department of Chemistry, University of Warwick, Coventry, CV4 7AL, UK.
  • Rodger A; Department of Chemistry, University of Warwick, Coventry, CV4 7AL, UK.
  • Costantini G; Department of Chemistry, University of Warwick, Coventry, CV4 7AL, UK.
  • Sadler PJ; Department of Chemistry, University of Warwick, Coventry, CV4 7AL, UK.
Angew Chem Int Ed Engl ; 55(31): 8909-12, 2016 07 25.
Article en En | MEDLINE | ID: mdl-27240103
ABSTRACT
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.
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Osmio / ADN de Neoplasias / Estructuras Metalorgánicas / Antineoplásicos Límite: Humans Idioma: En Revista: Angew Chem Int Ed Engl Año: 2016 Tipo del documento: Article País de afiliación: Reino Unido
Texto completo
Imprimir
XML
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Osmio / ADN de Neoplasias / Estructuras Metalorgánicas / Antineoplásicos Límite: Humans Idioma: En Revista: Angew Chem Int Ed Engl Año: 2016 Tipo del documento: Article País de afiliación: Reino Unido