The effect of docosahexaenoic acid moiety on the cytotoxic activity of 1,2,4-thiadiazole derivatives

Among 3-(2-aminopropyl)-1,2,4-thiadiazole derivatives containing substitutable secondary amino group and exhibiting cytotoxic activity towards rat C6 glioma cells three compounds with LD50values ranged from 6 to 48 μM have been chosen. For these compounds amides with docosahexaenoic acid were synthesized and their cytotoxic activity was studied. It was shown that, although docosahexaenoic acid itself was not toxic for C6 glioma cells, its addition to the amino derivatives of 1,2,4-thiadiazole increased or decreased their cytotoxicity. These results demonstrate that acylation of cytotoxic compounds with docosahexaenoic acid does not necessarily lead to the increase of their activity and sometimes can inactivate a parent compound. This fact should be taken into consideration because of possibility of biological attachment of docosahexaenoic acid to the amino group of anti-cancer drugs. © 2014 Pleiades Publishing, Ltd.

Akimov MG, Gretskaya NM, Karnoukhova VA, Serkov IV, Proshin AN, Shtratnikova VY, Bezuglov VV

IBCH: 4151
Ссылка на статью в журнале: http://link.springer.com/10.1134/S1990750814010028
Кол-во цитирований на 12.2023: 3
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