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Design of conjugates based on sesquiterpene lactones with polyalkoxybenzenes by “click” chemistry to create potential anticancer agentsстатья
- Авторы: Neganova M.E., Smirnova E.V., Sharova E.V., Artyushin O.I., Aleksandrova Yu R., Yandulova E.Yu, Nikolaeva N.S., Brel V.K.
- Журнал: Molecules
- Том: 27
- Номер: 23
- Год издания: 2022
- Издательство: MDPI
- Местоположение издательства: Basel, Switzerland
- Первая страница: 8411
- DOI: 10.3390/molecules27238411
- Аннотация: Using the methodology of “click” chemistry, a singular method has been developed forthe synthesis of unique conjugates based on sesquiterpene lactones: dehydrocostuslactone andalantolactone with polyalkoxybenzenes. To expand the structural range of the resulting conjugates,the length of the 1,2,3-triazole spacer was varied. For all synthesized compounds, the cytotoxic profile was determined on the cell lines of tumor origin (SH-SY5Y, HeLa, Hep-2, A549) and normal Hek 293 cells. It was found that the compounds based on alantolactone 7a–d with a long spacer and substances containing dehydrocostuslactone 10a–d with a short spacer have the greatest toxic effect. The decrease in cell survival under the action of these conjugates may be due to their ability to cause dissipation of the transmembrane potential of mitochondria and inhibit the process of glycolysis, leading to cell death. The obtained results confirm the assumption that the development of conjugates based on sesquiterpene lactones and polyalkoxybenzenes can be considered as a promising strategy for the search for potential antitumor agents.
- Добавил в систему: Смирнова Екатерина Владимировна
Прикрепленные файлы
| № | Имя | Описание | Имя файла | Размер | Добавлен |
|---|---|---|---|---|---|
| 1. | Полный текст | статья | molecules-27-08411.pdf | 2,6 МБ | 12 декабря 2022 [SmirnovaEV112] |
| 2. | экспертное | Eksp_Molec_2022.pdf | 385,2 КБ | 12 декабря 2022 [SmirnovaEV112] |