title: Ruthenium(II) polypyridyl complexes with 1,8-naphthalimide group as DNA binder, photonuclease, and dual inhibitors of topoisomerases I and IIα.
abstract: Two ruthenium(II) polypyridyl complexes containing 1,8-naphthalimide group as DNA binders, photonucleases, and inhibitors of topoisomerases I and IIα are evaluated. The binding properties of [Ru(phen)2(pnip)]2+{1; phen=1,10-phenanthroline; pnip=12-[N-(p-phenyl)-1,8-napthalimide]- imidazo[4',5'-f] [1,10]phenanthroline} and [Ru(bpy)2(pnip)]2+(2; bpy=2,2'-bipyridine) with calf thymus DNA increases with increasing the bulkiness and hydrophobic character of ancillary ligands, although the two complexes possess high affinities for DNA via intercalation. Moreover, photoirradiation (λ=365nm) of the two complexes are found to induce strand cleavage of closed circular pBR322 plasmid DNA via singlet oxygen mechanism, while complex 1 displays more effective photocleavage activity than complex 2 under the same conditions. Topoisomerase inhibition and DNA strand passage assay reflect that complexes 1 and 2 are efficient dual poisons of topoisomerases I and IIα.
authors.affiliation: College of Chemistry, Xiangtan University, Xiangtan, PR China.
authors.forename: Yanmei
authors.initials: Y
authors.lastname: Sun
authors.affiliation: College of Chemistry, Xiangtan University, Xiangtan, PR China.
authors.forename: Jia
authors.initials: J
authors.lastname: Li
authors.affiliation: College of Chemistry, Xiangtan University, Xiangtan, PR China.
authors.forename: Hong
authors.initials: H
authors.lastname: Zhao
authors.affiliation: Key Lab of Environment-Friendly Chemistry and Application in Ministry of Education, Xiangtan University, Xiangtan, PR China. Electronic address: lfwyxh@yeah.net.
authors.forename: Lifeng
authors.initials: L
authors.lastname: Tan
mesh_terms: D000951:Antigens, Neoplasm / Q000737:chemistry*; D004247:DNA / Q000737:chemistry*; D004264:DNA Topoisomerases, Type I / Q000737:chemistry*; D004250:DNA Topoisomerases, Type II / Q000737:chemistry*; D004268:DNA-Binding Proteins / Q000737:chemistry*; D053644:Naphthalimides / Q000138:chemical synthesis / Q000737:chemistry; D012428:Ruthenium / Q000737:chemistry*; D059003:Topoisomerase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry
chemical_list: D000951:Antigens, Neoplasm; D004268:DNA-Binding Proteins; D053644:Naphthalimides; D059003:Topoisomerase Inhibitors; D012428:Ruthenium; D004247:DNA; D004264:DNA Topoisomerases, Type I; D004250:DNA Topoisomerases, Type II
keywords: DNA binding; Photocleavage; Ruthenium(II) complexes; Topoisomerase inhibition