Результаты исследований: Научные публикации в периодических изданиях › статья › Рецензирование
A series of analogs of the earlier reported lead compound DVD-445 (thioredoxin reductase inhibitor with anticancer activity) has been synthesized via a modified Ugi reaction and investigated. Seven most potent compounds (with IC50 below 5.00 μM against recombinant rTrxR1 enzyme) were examined for their effect on cell growth and viability, oxidative stress induction and P-glycoprotein (P-gp) inhibition in human glioblastoma cells cell line U87 and its corresponding multidrug resistant (MDR) cell line U87-TxR. Several of these frontrunner compounds were shown to be superior over DVD-445. Besides providing promising candidates for anticancer therapy, our study further validates the small electrophilic Ugi Michael acceptor (UMA) chemotype as efficacious inhibitor of thioredoxin reductase.
Язык оригинала | английский |
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Номер статьи | 112119 |
Число страниц | 11 |
Журнал | European Journal of Medicinal Chemistry |
Том | 191 |
Дата раннего онлайн-доступа | 6 фев 2020 |
DOI | |
Состояние | Опубликовано - 1 апр 2020 |
ID: 51913267