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Synthesis of the first morpholine-containing iron(II) clathrochelates: A new class of efficient functionalized transcription inhibitorsстатья
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 марта 2017 г.
- Авторы: Belov Alexander S., Vologzhanina Anna V., Novikov Valentin V., Negrutska Valentina V., Dubey Igor Y., Mikhailova Zoya A., Lebed Ekaterina G., Voloshin Yan Z.
- Журнал: Inorganica Chimica Acta
- Том: 421
- Год издания: 2014
- Издательство: Elsevier BV
- Местоположение издательства: Netherlands
- Первая страница: 300
- Последняя страница: 306
- DOI: 10.1016/j.ica.2014.06.016
- Аннотация: Nucleophilic substitution of an iron(II) dichloroclathrochelate with morpholine as a N-nucleophilic agent afforded a monomorpholine-containing cage complex, characterized by X-ray diffraction. This complex as a monochloroclathrochelate precursor easily undergoes further nucleophilic substitution with 2-ethanolamine as a N-nucleophile and with meta- and para-mercaptobenzoic acids as S-nucleophiles, giving the bifunctional N,N- and N,S-substituted macrobicyclic iron(II) complexes. In vitro testing in a transcription assay based on T7 RNA polymerase showed the efficient structure- and concentration-dependent inhibition of transcription by these heterofunctionalized cage compounds in low- and submicromolar concentration range. The proposed mode of inhibition includes a trapping of clathrochelate inhibitor molecule by the binding pocket formed by three interconnected macromolecules of the transcription complex.
- Добавил в систему: Вологжанина Анна Владимировна