title: DNA binding and topoisomerase II inhibitory activity of water-soluble ruthenium(II) and rhodium(III) complexes.
abstract: Water-soluble piano-stool arene ruthenium complexes based on 1-(4-cyanophenyl)imidazole (CPI) and 4-cyanopyridine (CNPy) with the formulas [(eta6-arene)RuCl2(L)] (L = CPI, eta6-arene = benzene (1), p-cymene (2), hexamethylbenzene (3); L = CNPy, eta6-arene = benzene (4), p-cymene (5), hexamethylbenzene (6)) have been prepared by our earlier methods. The molecular structure of [(eta6-C6Me6)RuCl2(CNPy)] (6) has been determined crystallographically. Analogous rhodium(III) complex [(eta5-C5Me5)RhCl2(CPI)] (7) has also been prepared and characterized. DNA interaction with the arene ruthenium complexes and the rhodium complex has been examined by spectroscopic and gel mobility shift assay; condensation of DNA and B-->Z transition have also been described. Arene ruthenium(II) and EPh3 (E = P, As)-containing arene ruthenium(II) complexes exhibited strong binding behavior, however, rhodium(III) complexes were found to be Topo II inhibitors with an inhibition percentage of 70% (7) and 30% (7a). Furthermore, arene ruthenium complexes containing polypyridyl ligands also act as mild Topo II inhibitors (10%, 3c and 40%, 3d) in contrast to their precursor complexes. Complexes 4-6 also show significant inhibition of beta-hematin/hemozoin formation activity.
authors.affiliation: Department of Chemistry, Faculty of Science, Banaras Hindu University, Varanasi-221005 (U.P.), India.
authors.forename: Sanjay Kumar
authors.initials: SK
authors.lastname: Singh
authors.forename: Shweta
authors.initials: S
authors.lastname: Joshi
authors.forename: Alok Ranjan
authors.initials: AR
authors.lastname: Singh
authors.forename: Jitendra Kumar
authors.initials: JK
authors.lastname: Saxena
authors.forename: Daya Shankar
authors.initials: DS
authors.lastname: Pandey
mesh_terms: D018360:Crystallography, X-Ray; D004247:DNA / Q000737:chemistry*; D004250:DNA Topoisomerases, Type II / Q000378:metabolism*; D008958:Models, Molecular; D012238:Rhodium / Q000737:chemistry* / Q000494:pharmacology*; D017975:Ruthenium Compounds / Q000737:chemistry* / Q000494:pharmacology*; D012995:Solubility; D059005:Topoisomerase II Inhibitors; D014867:Water / Q000737:chemistry
chemical_list: D017975:Ruthenium Compounds; D059005:Topoisomerase II Inhibitors; D014867:Water; D004247:DNA; D012238:Rhodium; D004250:DNA Topoisomerases, Type II