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Effect of ancillary ligands on the topoisomerases II and transcription inhibition activity of polypyridyl ruthenium(II) complexes by Xing Chen; Feng Gao; Zhu-Xin Zhou; Wei-Yan Yang; Li-Tian Guo; Liang-Nian Ji is a Chemistry article available to read on EtoBox.

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To explore the structure-activity relationship of polypyridyl ruthenium(II) complexes as topoisomerase II and T7 RNA polymerase inhibitors, four new complexes, [Ru(4dmb)(2)(ppd)](2+) (4dmb=4,4'-dimethyl-2,2'-bipyridine, ppd=pteridino[6,7-f][1,10] phenanthroline-1,13(10H,12H)-dione), [Ru(5dmb)(2)(ppd)](2+) (5dmb=5,5'-dimethyl-2,2'-bipyridine), [Ru(dip)(2)(ppd)](2+) (dip=4,7-diphenyl-1,10-phenanthroline), and [Ru(ip)(2)(ppd)](2+) (ip=imidazole[4,5-f][1,10]phenanthroline) have been synthesized and characterized in detail by (1)H NMR spectroscopy, mass spectrometry and elemental analysis. Their interaction with calf thymus DNA and the inhibitory activity towards topoisomerase II and T7 RNA polymerase were investigated. The results suggest that although all of these four Ru(II) complexes are potent DNA intercalators, topoisomerase II inhibitors and DNA transcription inhibitors, their DNA binding strength and inhibitory activities are quite different. The activity of ip- and dip-complexes are significantly higher than the dmb-complexes. To explain the experimental regularity and reveal the underlying quantum chemistry mechanism of the biological activity, the properties of energy levels

Who reads Effect of ancillary ligands on the topoisomerases II and transcription inhibition activity of polypyridyl ruthenium(II) complexes?

Author

Xing Chen; Feng Gao; Zhu-Xin Zhou; Wei-Yan Yang; Li-Tian Guo; Liang-Nian Ji

Publisher

Elsevier Science; Elsevier ; Elsevier BV (ISSN 0162-0134)

Published

2010

Language

EN

Field

Chemistry (Physical Sciences)