1. Shemyakin–Ovchinnikov Institute of Bioorganic Chemistry Russian Academy of Sciences 2. Institute of Physiologically Active Compounds Russian Academy of Sciences 3. Innovative Technological Center “Biologically Active Compounds and their Applications”
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: docosahexaenoic acid, 1,2,4-thiadiazoles, rat C6 glioma
Akimov M.G. et al. The influence of docosahexaenoic acid moiety on cytotoxic activity of 1,2,4-thiadiazole derivatives // Biomeditsinskaya khimiya. - 2014. - V. 60. -N 4. - P. 473-478.
Akimov M.G. et al., "The influence of docosahexaenoic acid moiety on cytotoxic activity of 1,2,4-thiadiazole derivatives." Biomeditsinskaya khimiya 60.4 (2014): 473-478.
Akimov, M. G., Gretskaya, N. M., Karnoukhova, V. A., Serkov, I. V., Proshin, A. N., Shtratnikova, V. Yu., Bezuglov, V. V. (2014). The influence of docosahexaenoic acid moiety on cytotoxic activity of 1,2,4-thiadiazole derivatives. Biomeditsinskaya khimiya, 60(4), 473-478.