The influence of docosahexaenoic acid moiety on cytotoxic activity of 1,2,4-thiadiazole derivatives
- 1 July 2014
- journal article
- english abstract
- Published by Institute of Biochemistry in Biomeditsinskaya Khimiya
- Vol. 60 (4), 473-478
- https://doi.org/10.18097/pbmc20146004473
Abstract
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.Keywords
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