Luminescent cyclometalated platinum(II) complex forms emissive intercalating adducts with double-stranded DNA and RNA: differential emissions and anticancer activities.
Angew Chem Int Ed Engl
; 53(38): 10119-23, 2014 Sep 15.
Article
em En
| MEDLINE
| ID: mdl-25044924
ABSTRACT
Luminescent metallo-intercalators are potent biosensors of nucleic acid structure and anticancer agents targeting DNAs. There are few examples of luminescent metallo-intercalators which can simultaneously act as emission probes of nucleic acid structure and display promising anticancer activities. Herein, we describe a luminescent platinum(II) complex, [Pt(C^N^N)(C≡NtBu)]ClO4 (1 a, HC^N^N= 6-phenyl-2,2'-bipyridyl), that intercalates between the nucleobases of nucleic acids, accompanied by an increase in emission intensity and/or a significant change in the maximum emission wavelength. The changes in emission properties measured with double-stranded RNA (dsRNA) are different from those with dsDNA used in the binding reactions. Complex 1 a exhibited potent anticancer activity towards cancer cells inâ
vitro and inhibited tumor growth in a mouse model. The stabilization of the topoisomeraseâ
I-DNA complex with resulting DNA damage by 1 a is suggested to contribute to its anticancer activity.
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Base de dados:
MEDLINE
Assunto principal:
Compostos Organoplatínicos
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DNA
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RNA de Cadeia Dupla
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Luminescência
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Neoplasias Experimentais
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Antineoplásicos
Limite:
Animals
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Humans
Idioma:
En
Ano de publicação:
2014
Tipo de documento:
Article