Synthesis and antitumor activity of new furyl-2-substituted 1,3,4-thiadiazoles and 1,2,4-triazoles

New S- And N- Substituted Derivatives Of 5-Aryloxymethyl-1,2,4-Triazoles And Their Biological Activity

“…Variation of substituents in the aromatic ring would make it possible to trace the change in biological properties and reveal a possible structure-activity relationship in the series of 3-aryloxymethylsubstituted 1,2,4-triazole-3-thiols 1-7. For this purpose, the latter were alkylated with chloroacetic acid, chloroacetamide, chloroethylacetate under the conditions we developed earlier [11]. In the ¹H NMR spectra of the reaction products, singlet signals of the protons of SCH2-groups appear in the region of 3.86-4.11 ppm, which, together with the data of the ¹³С NMR spectra, confirm the alkylation reaction at the SH group of triazoles 1-7.…”

Новые 3-(4-пропоксибензил)-5-сульфанилзамещенные (4<I>H</I>)-1,2,4-триазолы и их противоопухолевая активность

“…Ðàíåå ìû ñîîáùàëè î ñèíòåçå ïðîèçâîäíûõ 1,2,4-òðèàçîëà, ñîäåðaeàùèõ â ïîëîaeåíèÿõ 3,4,5 ãåòåðîöèêëà ôàðìàêîôîðíûå ôðàãìåíòû, ñ öåëüþ ïîèñêà ñðåäè íèõ íîâûõ áèîëîãè÷åñêè àêòèâíûõ ñîåäèíåíèé.  ÷àñòíîñòè, âûÿâëåíû ñîåäèíåíèÿ ñ óìåðåííûìè èëè âûðàaeåííûìè ãèïîãëèêåìè÷åñêèìè [1,2], ìóòàãåííûìè [3], âëèÿþùèìè íà ìåòèëèðîâàíèå ÄÍÊ [4] è ïðîòèâîîïóõîëåâûìè [5,6] ñâîéñòâàìè. Íàñòîÿùàÿ ðàáîòà ÿâëÿåòñÿ ïðîäîëaeåíèåì ýòèõ èññëåäîâàíèé, ïîçâîëÿþùèõ ðàñøèðèòü âîçìîaeíîñòü ïîèñêà íîâûõ ýôôåêòèâíûõ áèîëîãè÷åñêè àêòèâíûõ ñðåäñòâ â óïîìÿíóòîì ðÿäó è ñïîñîáñòâîâàòü âûÿâëåíèþ âîçìîaeíîé çàâèñèìîñòè ñòðóêòóðà -àêòèâíîñòü ïðè ââåäåíèè 4-ïðîïîêñèáåíçèëüíîãî çàìåñòèòåëÿ â ïîëîaeåíèå 3 ãåòåðîöèêëà.…”