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Transferring the concept of multinuclearity to ruthenium complexes for improvement of anticancer activityстатья
Статья опубликована в высокорейтинговом журнале
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 июля 2013 г.
- Авторы: Mendoza-Ferri M.G., Hartinger C.G., Mendoza M.A., Groessl M., Egger A.E., Eichinger R.E., Mangrum J.B., Farrell N.P., Maruszak M., Bednarski P.J., Klein F., Jakupec M.A., Nazarov A.A., Severin K., Keppler B.K.
- Журнал: Journal of Medicinal Chemistry
- Том: 52
- Номер: 4
- Год издания: 2009
- Издательство: American Chemical Society
- Местоположение издательства: United States
- Первая страница: 916
- Последняя страница: 925
- DOI: 10.1021/jm8013234
- Аннотация: Multinuclear platinum anticancer complexes are a proven option to overcome resistance of established anticancer compounds. Transferring this concept to ruthenium complexes led to the synthesis of dinuclear Ru(II)-arene compounds containing a bis(pyridinone)alkane ligand linker. A pronounced influence of the spacer length on the in vitro anticancer activity was found, which is correlated to the lipophilicity of the complexes. IC50 values in the same dimension as for established platinum drugs were found in human tumor cell lines. No cross-resistance to oxoplatin, a cisplatin prodrug, was observed for the most active complex in three resistant cell lines; in fact, a 10-fold reversal of sensitivity in two of the oxoplatin-resistant lines was found. (Bio)analytical characterization of the representative examples showed that the ruthenium complexes hydrolyze rapidly, forming predominantly diaqua species that exhibit affinity toward transferrin and DNA, indicating that both proteins and nucleobases are potential targets. © 2009 American Chemical Society.
- Добавил в систему: Назаров Алексей Анатольевич