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

Akimov M.G.1 , Gretskaya N.M.1, Karnoukhova V.A.1, Serkov I.V.2, Proshin A.N.2, Shtratnikova V.Yu.3, Bezuglov V.V.1

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”
Section: Experimental Study
DOI: 10.18097/PBMC20146004473      PubMed Id: 25249531
Year: 2014  Volume: 60  Issue: 4  Pages: 473-478
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.
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Keywords: docosahexaenoic acid, 1,2,4-thiadiazoles, rat C6 glioma

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.
This paper is also available as the English translation: 10.1134/S1990750814010028
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