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N-glycosides indolo[2,3,-a]pyrrolo[3,4,-c]carbazole derivatives chemical structure influence on antitumor activityстатья
- Авторы: Kiseleva M.P., Pokrovsky V.S., Borisova L.M., Golubeva I.S., Ektova L.V.
- Журнал: Molecules
- Том: 18
- Номер: 2
- Год издания: 2019
- Издательство: MDPI
- Местоположение издательства: Basel, Switzerland
- Первая страница: 32
- Последняя страница: 39
- DOI: 10.17650/1726-9784-2019-18-2-32-39
- Аннотация: Introduction . The report considers the prospect of rational approach to the new anticancer agents creation based on indolocarbazole derivatives.Objective . To conduct a comparative study of 12 domestic N-glycosides, indolo[2,3-a]pirrolo[2,3-a]carbazole derivatives in the courseof “structure – activity” bond analysis.Materials and methods . The investigation of influence of 12 carbohydrate – containing indolocarbazoles, synthesized in N. N. BlokhinRussian Cancer Research Center of the Ministry of Health of Russia, performed on models of solid transplantable mouse tumors: lung Lew-is epidermoid carcinoma and B16 melanoma. The antitumor effect was assessed by Lewis epidermoid carcinoma and B16 melanomatumor growth inhibition (TGI %) criterion.Results . A variety of indolocarbazoles modifications allowed revealing the dependence of their antitumor properties on the structureof both, the aglycone and the glycoside residue. Imino-nitrogen interchange of atoms in upper heterocycle influences on indocarbazolederivatives antitumor activity change. During a comparative study of 12 N-glycosides indolocarbazole derivatives on lung Lewis epider-moid carcinoma and B16 melanoma models, 8 derivatives showed antitumor activity.Conclusion . The formulated concepts on the modification features in indolocarbazole derivatives structure can be used for more activecompounds creation with greater action selectivity.
- Добавил в систему: Пугачева Ружена Борисовна