Synthesis and cytotoxicity evaluation of naphthalimide derived N-mustards.
Molecules
; 19(7): 8803-19, 2014 Jun 25.
Article
em En
| MEDLINE
| ID: mdl-24968335
ABSTRACT
A series of N-mustards, which was conjugated to mono- or bis-naphthalimides with a flexible amine link, were synthesized and evaluated for cytotoxicity against five cancer cell lines (HCT-116, PC-3, U87 MG, Hep G2 and SK-OV-3). Several compounds displayed better activities than the control compound amonafide. Further evaluations by fluorescence spectroscopy studies and DNA-interstrand cross-linking assays revealed that the derivatives showed both alkylating and intercalating properties. Among the derivatives, the bis-naphthalimide N-mustard derivative 11b was found to exhibit the highest cytotoxic activity and DNA cross-linking ability. Both 11b and 7b induce HCT-116 cell apoptosis by S phase arrest.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Mostardas de Fosforamida
/
Antineoplásicos Alquilantes
/
Naftalimidas
Limite:
Humans
Idioma:
En
Revista:
Molecules
Ano de publicação:
2014
Tipo de documento:
Article