[The influence of docosahexaenoic acid moiety on cytotoxic activity of 1,2,4-thiadiazole derivatives].
In: Biomeditsinskaia khimiia, Jg. 60 (2014-07-01), Heft 4, S. 473-8
academicJournal
Zugriff:
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.
Titel: |
[The influence of docosahexaenoic acid moiety on cytotoxic activity of 1,2,4-thiadiazole derivatives].
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Autor/in / Beteiligte Person: | Akimov, MG ; Gretskaia, NM ; Karnoukhova, VA ; Serkov, IV ; Proshin, AN ; VIu, Shtratnikova ; Bezuglov, VV |
Zeitschrift: | Biomeditsinskaia khimiia, Jg. 60 (2014-07-01), Heft 4, S. 473-8 |
Veröffentlichung: | Moskva : Rossiĭskai︠a︡ akademii︠a︡ medit︠s︡inskikh nauk, 2003-, 2014 |
Medientyp: | academicJournal |
ISSN: | 2310-6972 (print) |
DOI: | 10.18097/pbmc20146004473 |
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