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New designed DNA light switch Ruthenium complexes as DNA photocleavers and Topoisomerase I inhibitors

Xue-Wen Liu,Yang Xiao,Wei-Gen Peng,Li-Jin Zhao,You-Ming Shen,Song-Bai Zhang,Ji-Lin Lu

Two ruthenium complexes containing a new ligand phipz (phipz = 2-(1,10-phenanthroline)-1H-imidazo[4,5-b]phenazine) were designed and synthesized. These complexes were found to inhibit the DNA supercoiled relaxation mediated by topoisomerase I (topo I), cleave DNA under irradiation and bind to calf thymus DNA through intercalative mode. Furthermore, complex 2 shows higher photocleavage activity, topo I inhibition activity and DNA affinity than complex 1 . Additionally, introduction of phenazine unit may be the reason that two complexes exhibit DNA ‘light switch’ behavior. The present work shows that two complexes might be potential as new DNA ‘light switches’, DNA photocleavers and topo I inhibitors.