Design, synthesis, and biological evaluation of substituted naphthalene imides and diimides as anticancer agent.
J Med Chem
; 52(23): 7873-7, 2009 Dec 10.
Article
em En
| MEDLINE
| ID: mdl-19954251
ABSTRACT
Naphthalimmide (NI) and 1,4,5,8-naphthalentetracarboxylic diimide (NDI) derivatives were synthesized and evaluated for their antiproliferative activity. NDI derivatives 1-9 were more cytotoxic than the corresponding NI derivatives 10-18. The molecular mechanisms of 1 and 2 were investigated in comparison to mitonafide. They interacted with DNA, were not topoisomerase IIalpha poisons, triggered caspase activation, caused p53 protein accumulation, and down-regulated AKT survival. Furthermore, 1 and 2 caused a decrease of ERK1/2 and, unlike mitonafide, inhibited ERKs phosphorylation.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Imidas
/
Naftalenos
/
Antineoplásicos
Idioma:
En
Ano de publicação:
2009
Tipo de documento:
Article