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3-Arylidene-2-oxindoles as GSK3β inhibitors and anti-thrombotic agentsстатья
Информация о цитировании статьи получена из
Scopus
Статья опубликована в журнале из списка Web of Science и/или Scopus
Дата последнего поиска статьи во внешних источниках: 1 мая 2024 г.
- Авторы: Babkov Denis, Bezsonova Elena, Sirotenko Viktor, Othman Elias, Klochkov Vladlen, Sosonyuk Sergey, Lozinskaya Natalia, Spasov Alexander
- Журнал: Bioorganic and Medicinal Chemistry Letters
- Том: 87
- Год издания: 2023
- Издательство: Pergamon Press Ltd.
- Местоположение издательства: United Kingdom
- Номер статьи: 129283
- DOI: 10.1016/j.bmcl.2023.129283
- Аннотация: Development of novel agents that prevent thrombotic events is an urgent task considering increasing incidence of cardiovascular diseases and coagulopathies that accompany cancer and COVID-19. Enzymatic assay identified novel GSK3β inhibitors in a series of 3-arylidene-2-oxindole derivatives. Considering the putative role of GSK3β in platelet activation, the most active compounds were evaluated for antiplatelet activity and antithrombotic activity. It was found that GSK3β inhibition by 2-oxindoles correlates with inhibition of platelet activation only for compounds 1b and 5a. Albeit, in vitro antiplatelet activity matched well with in vivo anti-thrombosis activity. The most active GSK3β inhibitor 5a exceeds antiplatelet activity of acetylsalicylic acid in vitro by 10.3 times and antithrombotic activity in vivo by 18.7 times (ED50 7.3 mg/kg). These results support the promising role of GSK3β inhibitors for development of novel antithrombotic agents.
- Добавил в систему: Лозинская Наталья Александровна