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Biomed Khim ; 60(4): 473-8, 2014.
Artículo en Ruso | MEDLINE | ID: mdl-25249531

RESUMEN

Among 3-(2-aminopropyl)-1,2,4-thiadiazole derivatives contatining substitution-ready secondary amino group and exhibiting cytotoxic towards rat C 6 glioma cells three compounds with LD 50 values ranged from 6 to 48 мM were chosen. For these compounds amides with docosahexaenoic acid were synthetised and their cytotoxic activity was studied. It was shown that, although docosahexaenoic acid itself was not toxic for C 6 glioma cells, its addition to the amino derivatives of 1,2,4-thiadiazole increased or decreased resultant cytotoxicity. The effect depended on the structure of 1,2,4-thiadiazole substituents. The obtained data show that the acylation of cytotoxic compounds with docosahexaenoic acid does not necessarily lead to the increase of their activity, but sometimes can inactivate a compound. This fact should be taken into account, especially in the case of anti-cancer drug development.


Asunto(s)
Amidas/farmacología , Antineoplásicos/farmacología , Citotoxinas/farmacología , Ácidos Docosahexaenoicos/química , Neuroglía/efectos de los fármacos , Tiadiazoles/farmacología , Amidas/síntesis química , Animales , Antineoplásicos/síntesis química , Línea Celular Tumoral , Citotoxinas/síntesis química , Diseño de Fármacos , Concentración 50 Inhibidora , Neuroglía/patología , Ratas , Relación Estructura-Actividad , Tiadiazoles/síntesis química
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