3-Arylidene-2-oxindoles as Potent NRH:Quinone Oxidoreductase 2 Inhibitors

Lozinskaya, N.A.; Bezsonova, E.N.; Dubar, M.; Melekhina, D.D.; Bazanov, D.R.; Bunev, A.S.; Grigor’eva, O.B.; Klochkov, V.G.; Sokolova, E.V.; Babkov, D.A.; Spasov, A.A.; Sosonyuk, S.E.

Авторы: Lozinskaya Natalia A., Bezsonova Elena N., Dubar Meriam, Melekhina Daria D., Bazanov Daniil R., Bunev Alexander S., Grigor’eva Olga B., Klochkov Vladlen G., Sokolova Elena V., Babkov Denis A., Spasov Alexander A., Sosonyuk Sergey E.
Журнал: Molecules
Том: 28
Номер: 3
Год издания: 2023
Издательство: MDPI
Местоположение издательства: Basel, Switzerland
Номер статьи: 1174
DOI: 10.3390/molecules28031174
Аннотация: The enzyme NRH:quinone oxidoreductase 2 (NQO2) plays an important role in the pathogenesis of various diseases such as neurodegenerative disorders, malaria, glaucoma, COVID-19 and cancer. NQO2 expression is known to be increased in some cancer cell lines. Since 3-arylidene-2-oxindoles are widely used in the design of new anticancer drugs, such as kinase inhibitors, it was interesting to study whether such structures have additional activity towards NQO2. Herein, we report the synthesis and study of 3-arylidene-2-oxindoles as novel NRH:quinone oxidoreductase inhibitors. It was demonstrated that oxindoles with 6-membered aryls in the arylidene moiety were obtained predominantly as E-isomers while for some 5-membered aryls, the Z-isomers prevailed. The most active compounds inhibited NQO2 with an IC50 of 0.368 µM. The presence of a double bond in the oxindoles was crucial for NQO2 inhibition activity. There was no correlation between NQO2 inhibition activity of the synthesized compounds and their cytotoxic effect on the A549 cell line.
Добавил в систему: Лозинская Наталья Александровна

	ИСТИНА	Войти в систему Регистрация
	ИСТИНА ЦЭМИ РАН
	Главная Поиск Статистика О проекте Помощь

ИСТИНА

ИСТИНА ЦЭМИ РАН

3-Arylidene-2-oxindoles as Potent NRH:Quinone Oxidoreductase 2 Inhibitorsстатья

Прикрепленные файлы