2,4,5-Tris(alkoxyaryl)imidazoline derivatives as potent scaffold for novel p53-MDM2 interaction inhibitors: Design, synthesis, and biological evaluation

Bazanov, D.R.; Pervushin, N.V.; Savitskaya, V.Y.; Anikina, L.V.; Proskurnina, M.V.; Lozinskaya, N.A.; Kopeina, G.S.

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: 18 сентября 2019 г.

Авторы: Bazanov Daniil R., Pervushin Nikolay V., Savitskaya Victoria Yu, Anikina Lada V., Proskurnina Marina V., Lozinskaya Natalia A., Kopeina Gelina S.
Журнал: Bioorganic and Medicinal Chemistry Letters
Том: 29
Номер: 16
Год издания: 2019
Издательство: Pergamon Press Ltd.
Местоположение издательства: United Kingdom
Первая страница: 2364
Последняя страница: 2368
DOI: 10.1016/j.bmcl.2019.06.007
Аннотация: Imidazoline-based small molecule inhibitors of p53-MDM2 interaction intended for the treatment of p53 wild-type tumors are the promising structures for design of anticancer drugs. Based on fragment approach we have investigated a key role of substituents in cis-imidazoline core for biological activity of nutlin family compounds. Although the necessity of the substituents in the phenyl rings of cis-imidazoline has been shown, there are no studies in which the replacements of a halogen by other substituents have been investigated. A series of simple cis-imidazoline derivatives containing halogen, hydroxy and alkoxy-substituents were synthesized. The biological activity of the compounds was studied using assays of cytotoxicity (MTT) and p53 level. It was found that the hydroxyl-derivatives were not cytotoxic whereas the alkoxy analogues were the same or more active as halogen-substituted compounds in cell viability test. The synthesized alkoxy derivatives induced an increase of p53 level and did not promote necrotic cell death in the concentration up to 40 µM.
Добавил в систему: Базанов Даниил Романович

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2,4,5-Tris(alkoxyaryl)imidazoline derivatives as potent scaffold for novel p53-MDM2 interaction inhibitors: Design, synthesis, and biological evaluationстатья Исследовательская статья

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