دورية أكاديمية
Arene–Ruthenium(II) Acylpyrazolonato Complexes: Apoptosis-Promoting Effects on Human Cancer Cells
| العنوان: | Arene–Ruthenium(II) Acylpyrazolonato Complexes: Apoptosis-Promoting Effects on Human Cancer Cells |
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| المؤلفون: | Anna Maria Eleuteri, Valentina Cecarini, Allan H. White, Claudio Pettinari, Laura Bonfili, Mauro Angeletti, Riccardo Pettinari, Massimo Nabissi, Massimiliano Cuccioloni, Matteo Mozzicafreddo, Brian W. Skelton, Fabio Marchetti |
| سنة النشر: | 2014 |
| المجموعة: | Istituto Nazionale di Fisica Nucleare (INFN): Open Access Repository |
| مصطلحات موضوعية: | Drug Discovery, Molecular Medicine |
| الوصف: | A series of ruthenium(II) arene complexes with the 4-(biphenyl-4-carbonyl)-3-methyl-1-phenyl-5-pyrazolonate ligand, and related 1,3,5-triaza-7-phosphaadamantane (PTA) derivatives, has been synthesized. The compounds have been characterized by NMR and IR spectroscopy, ESI mass spectrometry, elemental analysis, and X-ray crystallography. Antiproliferative activity in four human cancer cell lines was determined by MTT assay, yielding dose- and cancer cell line-dependent IC50 values of 9-34 μM for three hexamethylbenzene-ruthenium complexes, whereas the other metal complexes were much less active. Apoptosis was the mechanism involved in the anticancer activity of such compounds. In fact, the hexamethylbenzene-ruthenium complexes activated caspase activity, with consequent DNA fragmentation, accumulation of pro-apoptotic proteins (p27, p53, p89 PARP fragments), and the concomitant down-regulation of antiapoptotic protein Bcl-2. Biosensor-based binding studies indicated that the ancillary ligands were critical in determining the DNA binding affinities, and competition binding experiments further characterized the nature of the interaction. |
| نوع الوثيقة: | article in journal/newspaper |
| اللغة: | English |
| العلاقة: | url:https://www.openaccessrepository.it/communities/itmirrorTest; https://www.openaccessrepository.it/record/91737Test |
| DOI: | 10.1021/jm500458c |
| الإتاحة: | https://doi.org/10.1021/jm500458cTest https://www.openaccessrepository.it/record/91737Test |
| حقوق: | info:eu-repo/semantics/openAccess |
| رقم الانضمام: | edsbas.8E292BAB |
| قاعدة البيانات: | BASE |
| DOI: | 10.1021/jm500458c |
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