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Farmaco ; 59(4): 297-305, 2004 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-15081347

RESUMEN

The multistep synthesis of a series of new substituted-benzothiazoles as hydrochloride or quaternary salts is described. 6-Amidino substituted 2-aminobenzothiazoles (5, 6), N-methyl-2-(4-cyanostyryl)benzothiazolium iodide (8), cyano-substituted-2-styrylbenzothiazoles (9-11) and amidino and bis-amidino-substituted 2-styrylbenzothiazoles (12-17) were prepared. The crystal structure of amidino derivative (6) was determined by single crystal X-ray analysis. All new prepared compounds were tested on the cytostatic activities against malignant cell lines: (SW620, colon carcinoma; Hep2, laryngeal carcinoma; HBL, melanoma; HeLa, cervical carcinoma and WI38, human normal fibroblasts). The compounds exerted a different inhibitory effect, depended on concentration and type of the cells. The best inhibitory effect was achieved with compounds (12-15), with slight differences among them. All of them inhibited the growth of examined tumor cell lines and also normal fibroblasts. Other examined compounds exhibited a moderate inhibitory effect, depending on type of the cells. Majority of them inhibited the growth of HeLa cells and WI38.


Asunto(s)
Inhibidores de Crecimiento/síntesis química , Inhibidores de Crecimiento/farmacología , Tiazoles/síntesis química , Tiazoles/farmacología , Benzotiazoles , División Celular/efectos de los fármacos , División Celular/fisiología , Línea Celular , Línea Celular Tumoral , Cristalización , Cristalografía por Rayos X/métodos , Relación Dosis-Respuesta a Droga , Evaluación Preclínica de Medicamentos/métodos , Fibroblastos/citología , Fibroblastos/efectos de los fármacos , Inhibidores de Crecimiento/química , Células HeLa , Humanos , Tiazoles/química
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