Synthesis and antitumor activity of novel nitrogen mustard-linked chalcones.
Arch Pharm (Weinheim)
; 346(4): 292-9, 2013 Apr.
Article
en En
| MEDLINE
| ID: mdl-23519571
A series of nitrogen mustard-linked chalcones were synthesized and evaluated for their antitumor activity in vitro against the K562 and HepG2 cell lines. The aldol condensation of [N,N-bis(chloroethyl)-3-amino]-acetophenone (2) with aromatic aldehydes afforded the nitrogen mustard-linked chalcones. Among the analogs tested, compounds 5e and 5k exhibited significant anti-proliferation activities against K562 cells with IC50 values of 2.55 and 0.61 µM, respectively, which revealed higher cell toxicity than the standard drugs cisplatin (IC50>200 µM) and adriamycin (IC50=14.88 µM). The methoxyl and N,N-dimethyl groups on the B-ring of the chalcone frame enhanced the inhibitory activities against both the K562 and HepG2 cell lines. The structure-activity relationship study indicated that the inhibitory activities significantly varied with the position(s) and species of the substituted group(s).
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Chalconas
/
Antineoplásicos
/
Compuestos de Mostaza Nitrogenada
Límite:
Humans
Idioma:
En
Revista:
Arch Pharm (Weinheim)
Año:
2013
Tipo del documento:
Article
Pais de publicación:
Alemania