In vitro transcription inhibition by ruthenium(II) polypyridyl complexes with electropositive ancillary ligands.
Inorg Chem
; 48(13): 5599-601, 2009 Jul 06.
Article
em En
| MEDLINE
| ID: mdl-19505113
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.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Piridinas
/
Transcrição Gênica
/
Compostos de Rutênio
Limite:
Humans
Idioma:
En
Revista:
Inorg Chem
Ano de publicação:
2009
Tipo de documento:
Article