Synthesis and antitumor activity of 5-substituted-2-(pyridyl)benzothiazole compounds / 药学学报
Acta Pharmaceutica Sinica
; (12): 83-88, 2013.
Article
en Zh
| WPRIM
| ID: wpr-235700
Biblioteca responsable:
WPRO
ABSTRACT
Fifteen novel 5-substituted-2-(pyridyl)benzothiazole compounds were designed and synthesized by simple hydrolization and condensation reaction of the 2-amino-5-substituent benzothiazole. Activities of these synthesized compounds were evaluated on Bcap-37, HCT-15 and HepG2 tumor cells in vitro by standard MTT assay. 5-Fluorouracil (5-FU) was used as the positive control. The results revealed that most of the new compounds had potent effects on Bcap-37, HCT-15 and HepG2 tumor cells, and had no or less effect on 293T and L02 normal cells. Particularly, compounds 1c and 2e exhibited better activities on HCT-15 and HepG2 cells with IC50 values of 41.59 and 38.65 micromol x L(-1), and 1i showed excellent activities on Bcap-37 and HepG2 cells with IC50 values of 46.63 and 23.51 micromol x L(-1), respectively. The structure-activity relationship of 5-substituted-2-(pyridyl)benzothiazole compounds were also discussed preliminarily.
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Asunto principal:
Farmacología
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Relación Estructura-Actividad
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Ensayos de Selección de Medicamentos Antitumorales
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Estructura Molecular
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Química
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Línea Celular Tumoral
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Proliferación Celular
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Benzotiazoles
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Antineoplásicos
Límite:
Humans
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Año:
2013
Tipo del documento:
Article