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Sulfonamide derivatives of cis-imidazolines as potent p53-MDM2/MDMX protein-protein interaction inhibitorsстатья Исследовательская статья
Информация о цитировании статьи получена из
Web of Science,
Scopus
Статья опубликована в журнале из списка Web of Science и/или Scopus
Дата последнего поиска статьи во внешних источниках: 10 ноября 2021 г.
- Авторы: Bazanov Daniil R., Pervushin Nikolay V., Savin Egor V., Tsymliakov Michael D., Maksutova Anita I., Sosonyuk Sergey E., Kopeina Gelina S., Lozinskaya Natalia A.
- Журнал: Medicinal Chemistry Research
- Том: 30
- Год издания: 2021
- Издательство: Birkhaeuser
- Местоположение издательства: United States
- Первая страница: 2216
- Последняя страница: 2227
- DOI: 10.1007/s00044-021-02802-w
- Аннотация: p53-MDM2/MDMX interaction inhibitors represent the prospective agents for targeted anticancer therapy in tumors expressing wild-type p53 protein. Imidazoline-based MDM2-targeted inhibitors of such type, nutlins, contain halogen-substituted phenyl rings, which dramatically decrease the solubility of compounds in water. The addition of suitable hydrophilic substituents in benzene rings and to imidazoline nitrogen can improve the compound’s water solubility. In this study, we have synthesized novel hydrophilic cis-2,4,5-tris(alkoxyphenyl)imidazolines and studied the influence of N-sulfonyl substituent on protein-protein interaction compared to unsubstituted alkoxy-compounds. The biological activity of the obtained compounds was studied using Western blot analysis on A549, RKO and SH-SY5Y cancer cell lines. It was found that the derivatives are able to inhibit MDM2/MDMX-p53 interaction, promote p53 stabilization and induce p21 expression in the concentrations from 500 nM.
- Добавил в систему: Базанов Даниил Романович
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