Antitumor activity of (-)-alpha-bisabolol-based thiosemicarbazones against human tumor cell lines.
Eur J Med Chem
; 45(7): 2987-93, 2010 Jul.
Article
em En
| MEDLINE
| ID: mdl-20413188
A series of thiosemicarbazones deriving from the natural sesquiterpene (-)-alpha-bisabolol were synthesized and tested against a panel of eight human tumor cell lines to evaluate their anti-tumor potential. Some of the compounds exhibited inhibitory effects on the growth of a wide range of cancer cell lines, but myeloid leukemia cells (K-562) were especially sensitive to all tested thiosemicarbazones (GI(50) 0.01-4.22 microM). Among the analogues, the ketone derivative 3l was the most active, exhibiting potent antitumoral activity (GI(50) 0.01 microM) and high selectivity for K-562 cells (deltaTGI 505). It also demonstrated high cytotoxicity, with an LC(50) of 1.55 microM for the K-562 cells, but it showed only moderate selectivity (deltaLC(50) 38.5 microM). Through structure-activity relationship studies, we identified some structural requirement for the antitumoral activity exhibited by these promising compounds.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Sesquiterpenos
/
Tiossemicarbazonas
/
Antineoplásicos
Limite:
Humans
Idioma:
En
Revista:
Eur J Med Chem
Ano de publicação:
2010
Tipo de documento:
Article
País de afiliação:
Brasil
País de publicação:
França