Cytotoxic activity of new acetoxycoumarin derivatives in cancer cell lines.
Anticancer Res
; 31(6): 2017-22, 2011 Jun.
Article
em En
| MEDLINE
| ID: mdl-21737617
ABSTRACT
BACKGROUND:
Coumarin and their derivatives are important and useful compounds with diverse pharmacological properties. In the present study, we evaluated the in vitro cytotoxic activity of new acetoxycoumarin derivatives 4-(7-methoxy-4-methyl-2-oxo-2H-chromen-3-yl)phenyl acetate (1), 4-(1-methyl-3-oxo-3H-benzo[f]chromen-2-yl)phenyl acetate (2), 4-(6-propionamido-4-methyl-2-oxo-2H-chromen-3-yl) phenyl acetate (3), 4-(7-acetoxy-2-oxo-4-phenyl-2H-chromen-3-yl)phenyl acetate (4), 4-(2-oxo-4-phenyl-2H-chromen-3-yl)phenyl acetate (5), 4-(6-bromo-2-oxo-4-phenyl-2H-chromen-3-yl)phenyl acetate (6), 4-(7-(diethylamino)-4-methyl-2-oxo-2H-chromen-3-yl)phenyl acetate (7), 4-(6,8-dibromo-4-methyl-2-oxo-2H-chromen-3-yl)phenyl acetate (8) against A549 human lung cancer, CRL 1548 rat liver cancer and CRL 1439 normal rat liver cells. MATERIALS ANDMETHODS:
The cytotoxic activity was evaluated by crystal violet dye-binding assay. The effect of compounds 5 and 7 on different phases of the cell cycle was determined using flow cytometry.RESULTS:
In the A549 lung cancer cell line, the 50% lethal dose (LD50) values for compounds 1-4, 6 and 8 were found to be >100 µM while those for 5 and 7 were 89.3 and 48.1 µM, respectively after 48 h treatment. In the CRL 1548 liver cancer cell line, only compound 7 showed toxicity, with an LD50 of 45.1 µM. Compounds 5 and 7 caused different cell phase arrest in lung and liver cancer cell lines.CONCLUSION:
The results indicate that 4-(7-(diethylamino)-4-methyl-2-oxo-2H-chromen-3-yl)phenyl acetate (7) had the highest cytotoxic activity in all of the examined cell lines.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Cumarínicos
/
Antineoplásicos
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Anticancer Res
Ano de publicação:
2011
Tipo de documento:
Article