Academic Journal
New Organometallic Ru(II) Compounds with Lonidamine Motif as Antitumor Agents
| العنوان: | New Organometallic Ru(II) Compounds with Lonidamine Motif as Antitumor Agents |
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| المؤلفون: | Ilya A. Shutkov, Yulia N. Okulova, Dmitrii M. Mazur, Nikolai A. Melnichuk, Denis A. Babkov, Elena V. Sokolova, Alexander A. Spasov, Elena R. Milaeva, Alexey A. Nazarov |
| المصدر: | Pharmaceutics, Vol 15, Iss 5, p 1366 (2023) |
| بيانات النشر: | MDPI AG, 2023. |
| سنة النشر: | 2023 |
| المجموعة: | LCC:Pharmacy and materia medica |
| مصطلحات موضوعية: | ruthenium compounds, lonidamine, antiproliferative activity, ligand exchange, mode of action, Pharmacy and materia medica, RS1-441 |
| الوصف: | The combination of one molecule of organic and metal-based fragments that exhibit antitumor activity is a modern approach in the search for new promising drugs. In this work, biologically active ligands based on lonidamine (a selective inhibitor of aerobic glycolysis used in clinical practice) were introduced into the structure of an antitumor organometallic ruthenium scaffold. Resistant to ligand exchange reactions, compounds were prepared by replacing labile ligands with stable ones. Moreover, cationic complexes containing two lonidamine-based ligands were obtained. Antiproliferative activity was studied in vitro by MTT assays. It was shown that the increase in the stability in ligand exchange reactions does not influence cytotoxicity. At the same time, the introduction of the second lonidamine fragment approximately doubles the cytotoxicity of studied complexes. The ability to induce apoptosis and caspase activation in tumour cell MCF7 was studied by employing flow cytometry. |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 15051366 1999-4923 |
| Relation: | https://www.mdpi.com/1999-4923/15/5/1366; https://doaj.org/toc/1999-4923 |
| DOI: | 10.3390/pharmaceutics15051366 |
| URL الوصول: | https://doaj.org/article/0bd7d89685c443d9b8dc0b254006d427 |
| رقم الانضمام: | edsdoj.0bd7d89685c443d9b8dc0b254006d427 |
| قاعدة البيانات: | Directory of Open Access Journals |
Full Text Finder | تدمد: | 15051366 19994923 |
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| DOI: | 10.3390/pharmaceutics15051366 |