New Ruthenium(II)–Letrozole Complexes as Anticancer Therapeutics
| Autor: | Dusica Maysinger, Cédric Doucet, Annie Castonguay, Michal Juhás |
|---|---|
| Rok vydání: | 2012 |
| Předmět: |
Curcumin
Cell Survival medicine.drug_class Antineoplastic Agents Breast Neoplasms Adenocarcinoma Pharmacology Crystallography X-Ray Ruthenium Structure-Activity Relationship Breast cancer Coordination Complexes Cell Line Tumor Nitriles Drug Discovery Autophagy medicine Humans Drug Interactions Viability assay Cytotoxicity Cell Proliferation Aromatase inhibitor Aromatase Inhibitors Chemistry Adenine Letrozole Stereoisomerism Triazoles medicine.disease Cell culture Cancer cell Molecular Medicine Female Drug Screening Assays Antitumor Glioblastoma medicine.drug |
| Zdroj: | Journal of Medicinal Chemistry. 55:8799-8806 |
| ISSN: | 1520-4804 0022-2623 |
| Popis: | Novel ruthenium-letrozole complexes have been prepared, and cell viability of two human cancer cell types (breast and glioblastoma) was determined. Some ruthenium compounds are known for their cytotoxicity to cancer cells, whereas letrozole is an aromatase inhibitor administered after surgery to post-menopausal women with hormonally responsive breast cancer. A significant in vitro activity was established for complex 5·Let against breast cancer MCF-7 cells and significantly lower activity against glioblastoma U251N cells. The activity of 5·Let was even higher than that of 4, a compound analogous to the well-known drug RAPTA-C. Results from the combination of 5·Let (or 4) with 3-methyladenine (3-MA) or with curcumin, respectively, revealed that the resultant cancer cell death likely involves 5·Let-induced autophagy. |
| Databáze: | OpenAIRE |
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