title: [The influence of docosahexaenoic acid moiety on cytotoxic activity of 1,2,4-thiadiazole derivatives].
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.
authors.forename: M G
authors.initials: MG
authors.lastname: Akimov
authors.forename: N M
authors.initials: NM
authors.lastname: Gretskaia
authors.forename: V A
authors.initials: VA
authors.lastname: Karnoukhova
authors.forename: I V
authors.initials: IV
authors.lastname: Serkov
authors.forename: A N
authors.initials: AN
authors.lastname: Proshin
authors.forename: V Iu
authors.initials: VIu
authors.lastname: Shtratnikova
authors.forename: V V
authors.initials: VV
authors.lastname: Bezuglov
mesh_terms: D000577:Amides / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D045744:Cell Line, Tumor; D003603:Cytotoxins / Q000138:chemical synthesis / Q000494:pharmacology*; D004281:Docosahexaenoic Acids / Q000737:chemistry*; D015195:Drug Design; D020128:Inhibitory Concentration 50; D009457:Neuroglia / Q000187:drug effects* / Q000473:pathology; D051381:Rats; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: D000577:Amides; D000970:Antineoplastic Agents; D003603:Cytotoxins; D013830:Thiadiazoles; D004281:Docosahexaenoic Acids
keywords: 1,2,4-thiadiazoles; docosahexaenoic acid; rat C6 glioma