title: In vitro transcription inhibition by ruthenium(II) polypyridyl complexes with electropositive ancillary ligands.
abstract: Three Ru(II) polypyridyl complexes with potential high DNA-binding ability have been designed and synthesized by extending the conjugated plane of the intercalative ligand and introducing electropositive pendants to the ancillary ligand. Spectral titration, DNA thermal denaturation, viscosity experiments, and quantum chemistry calculations were performed, and the complexes were found to intercalate into DNA base pairs with very high affinity even at high salt concentrations. Benefiting from their high DNA-binding ability, the complexes can effectively inhibit the DNA transcription activity by blocking the binding of T7 RNA polymerase to the template DNA. As efficient transcription inhibitors, the complexes demonstrated high in vitro antitumor activity against four selected tumor cell lines.
authors.affiliation: MOE Laboratory of Bioinorganic and Synthetic Chemistry, State Key Laboratory of Optoelectronic Materials and Technologies, School of Chemistry and Chemical Engineering, Sun Yat-Sen University, Guangzhou 510275, PR China. gaofeng9@mail.sysu.edu.cn
authors.forename: Feng
authors.initials: F
authors.lastname: Gao
authors.forename: Xing
authors.initials: X
authors.lastname: Chen
authors.forename: Jin-Quan
authors.initials: JQ
authors.lastname: Wang
authors.forename: Yu
authors.initials: Y
authors.lastname: Chen
authors.forename: Hui
authors.initials: H
authors.lastname: Chao
authors.forename: Liang-Nian
authors.initials: LN
authors.lastname: Ji
mesh_terms: D045744:Cell Line, Tumor; D006801:Humans; D008024:Ligands; D011725:Pyridines / Q000737:chemistry*; D011789:Quantum Theory; D017975:Ruthenium Compounds / Q000737:chemistry / Q000494:pharmacology*; D014158:Transcription, Genetic / Q000187:drug effects*
chemical_list: D008024:Ligands; D011725:Pyridines; D017975:Ruthenium Compounds