Novel Pt(ii) complexes with modified aroyl-hydrazone Schiff-base ligands: synthesis, cytotoxicity and action mechanism.
Metallomics
; 11(11): 1847-1863, 2019 11 01.
Article
en En
| MEDLINE
| ID: mdl-31553341
ABSTRACT
To develop new anti-tumour Pt(ii) agents, we designed and synthesized five Pt(ii) complexes. These Pt(ii) complexes were modified benzene rings of 2-hydroxybenzylidene with a hydrocarbyl or halogen group. The five Pt(ii) complexes possessed remarkable cytotoxicity against tumour cells in vitro. In particular, we investigated chemotherapeutic mechanisms of the complexes against A549cisR cells. The Pt(ii) complexes could bind to and cleave DNA, while also inducing arrest of the cell cycle in S phase, leading to down-regulation of the levels of cyclin-dependent kinases and cyclin and up-regulation of the expression of p21. The selected complex, C3, changed the mitochondrial membrane potential and induced apoptosis. C3 also inhibited the expression of the c-myc gene and downstream proteins, thereby inhibiting telomerase activity.
Texto completo:
1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Platino (Metal)
/
Bases de Schiff
/
Hidrazonas
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Metallomics
Asunto de la revista:
BIOQUIMICA
Año:
2019
Tipo del documento:
Article