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Os 2 –Os 4 Switch Controls DNA Knotting and Anticancer Activity
Author(s) -
Fu Ying,
Romero María J.,
Salassa Luca,
Cheng Xi,
Habtemariam Abraha,
Clarkson Guy J.,
Prokes Ivan,
Rodger Alison,
Costantini Giovanni,
Sadler Peter J.
Publication year - 2016
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201602995
Subject(s) - osmium , biological activity , dna , chemistry , imine , metallacycle , dna condensation , plasmid , stereochemistry , combinatorial chemistry , biophysics , crystallography , biology , biochemistry , physics , in vitro , catalysis , x ray crystallography , transfection , ruthenium , diffraction , optics , gene
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.