PO-017 Oxorhenium(V) complexes in the drug combination study
Аутори
Petrović, TamaraGligorijević, Nevenka
Belaj, Ferdinand
Grgurić-Šipka, Sanja
Nikolić, Stefan
Krstić, Milena
Poljarević, Jelena
Mihajlović-Lalić, Ljiljana
Конференцијски прилог (Објављена верзија)
Метаподаци
Приказ свих података о документуАпстракт
Rhenium complexes merit particular attention in the area of metallodrug design due to rhenium’s broad spectrum of oxidation states and consequently, the possibility to design compounds of a great structural diversity. Thus, the synthesis, chemical characterization and antitumor activity in vitro of the three Re(V) complexes is described. Novel compounds were obtained via reaction of [ReOCl3(PPh3)2] with corresponding ligands (pyridine-2-carboxylic acid, 3-methylpyridine-2-carboxylic acid and 6-methylpyridine- 2-carboxylic acid) in acetonitrile at 78 °C for 3h. The complexes were fully characterized using NMR, IR, MS and elemental analysis. Their octahedral geometry with bidentate N^O ligand was confirmed by X-ray diffraction analysis. Antiproliferative effect was determined by MTT assay and only the complex with pyridine-2-carboxylic acid (1) showed dose-dependent cytotoxic potential, particularly toward triple-negative breast adenocarcinoma cells MDA-MB-231 with IC50 68.90 ±
1.73 μM ...and pancreatic adenocarcinoma cells PANC-1 with IC50 69.8 ± 2.3 μM. Drug combination studies in PANC-1 cells with 1 and Verapamil hydrochloride (VRP) showed slight arrest of cell cycle in the S phase and also it increase its antiproliferative potential to IC50 51.4 ± 2.8 μM. Part of the research included a depletion of the glutathione (GSH) level by L-buthionine-sulfoximine (L-BSO) at sub-toxic concentrations (100 μM) in PANC-1 cells which caused an increase of activity of 1 to the IC50 57.67 ± 6.51 μM.
Извор:
Österreichische Chemische Gesellschaft, September 20, 22, 2022, Vienna, Austria, 2022, 90-90Издавач:
- Wien, Österreich : Nibelungengasse
Напомена:
- Book of Abstracts
Колекције
Институција/група
Inovacioni centar / Innovation CentreTY - CONF AU - Petrović, Tamara AU - Gligorijević, Nevenka AU - Belaj, Ferdinand AU - Grgurić-Šipka, Sanja AU - Nikolić, Stefan AU - Krstić, Milena AU - Poljarević, Jelena AU - Mihajlović-Lalić, Ljiljana PY - 2022 UR - http://cherry.chem.bg.ac.rs/handle/123456789/5865 AB - Rhenium complexes merit particular attention in the area of metallodrug design due to rhenium’s broad spectrum of oxidation states and consequently, the possibility to design compounds of a great structural diversity. Thus, the synthesis, chemical characterization and antitumor activity in vitro of the three Re(V) complexes is described. Novel compounds were obtained via reaction of [ReOCl3(PPh3)2] with corresponding ligands (pyridine-2-carboxylic acid, 3-methylpyridine-2-carboxylic acid and 6-methylpyridine- 2-carboxylic acid) in acetonitrile at 78 °C for 3h. The complexes were fully characterized using NMR, IR, MS and elemental analysis. Their octahedral geometry with bidentate N^O ligand was confirmed by X-ray diffraction analysis. Antiproliferative effect was determined by MTT assay and only the complex with pyridine-2-carboxylic acid (1) showed dose-dependent cytotoxic potential, particularly toward triple-negative breast adenocarcinoma cells MDA-MB-231 with IC50 68.90 ± 1.73 μM and pancreatic adenocarcinoma cells PANC-1 with IC50 69.8 ± 2.3 μM. Drug combination studies in PANC-1 cells with 1 and Verapamil hydrochloride (VRP) showed slight arrest of cell cycle in the S phase and also it increase its antiproliferative potential to IC50 51.4 ± 2.8 μM. Part of the research included a depletion of the glutathione (GSH) level by L-buthionine-sulfoximine (L-BSO) at sub-toxic concentrations (100 μM) in PANC-1 cells which caused an increase of activity of 1 to the IC50 57.67 ± 6.51 μM. PB - Wien, Österreich : Nibelungengasse C3 - Österreichische Chemische Gesellschaft, September 20, 22, 2022, Vienna, Austria T1 - PO-017 Oxorhenium(V) complexes in the drug combination study SP - 90 EP - 90 UR - https://hdl.handle.net/21.15107/rcub_cherry_5865 ER -
@conference{ author = "Petrović, Tamara and Gligorijević, Nevenka and Belaj, Ferdinand and Grgurić-Šipka, Sanja and Nikolić, Stefan and Krstić, Milena and Poljarević, Jelena and Mihajlović-Lalić, Ljiljana", year = "2022", abstract = "Rhenium complexes merit particular attention in the area of metallodrug design due to rhenium’s broad spectrum of oxidation states and consequently, the possibility to design compounds of a great structural diversity. Thus, the synthesis, chemical characterization and antitumor activity in vitro of the three Re(V) complexes is described. Novel compounds were obtained via reaction of [ReOCl3(PPh3)2] with corresponding ligands (pyridine-2-carboxylic acid, 3-methylpyridine-2-carboxylic acid and 6-methylpyridine- 2-carboxylic acid) in acetonitrile at 78 °C for 3h. The complexes were fully characterized using NMR, IR, MS and elemental analysis. Their octahedral geometry with bidentate N^O ligand was confirmed by X-ray diffraction analysis. Antiproliferative effect was determined by MTT assay and only the complex with pyridine-2-carboxylic acid (1) showed dose-dependent cytotoxic potential, particularly toward triple-negative breast adenocarcinoma cells MDA-MB-231 with IC50 68.90 ± 1.73 μM and pancreatic adenocarcinoma cells PANC-1 with IC50 69.8 ± 2.3 μM. Drug combination studies in PANC-1 cells with 1 and Verapamil hydrochloride (VRP) showed slight arrest of cell cycle in the S phase and also it increase its antiproliferative potential to IC50 51.4 ± 2.8 μM. Part of the research included a depletion of the glutathione (GSH) level by L-buthionine-sulfoximine (L-BSO) at sub-toxic concentrations (100 μM) in PANC-1 cells which caused an increase of activity of 1 to the IC50 57.67 ± 6.51 μM.", publisher = "Wien, Österreich : Nibelungengasse", journal = "Österreichische Chemische Gesellschaft, September 20, 22, 2022, Vienna, Austria", title = "PO-017 Oxorhenium(V) complexes in the drug combination study", pages = "90-90", url = "https://hdl.handle.net/21.15107/rcub_cherry_5865" }
Petrović, T., Gligorijević, N., Belaj, F., Grgurić-Šipka, S., Nikolić, S., Krstić, M., Poljarević, J.,& Mihajlović-Lalić, L.. (2022). PO-017 Oxorhenium(V) complexes in the drug combination study. in Österreichische Chemische Gesellschaft, September 20, 22, 2022, Vienna, Austria Wien, Österreich : Nibelungengasse., 90-90. https://hdl.handle.net/21.15107/rcub_cherry_5865
Petrović T, Gligorijević N, Belaj F, Grgurić-Šipka S, Nikolić S, Krstić M, Poljarević J, Mihajlović-Lalić L. PO-017 Oxorhenium(V) complexes in the drug combination study. in Österreichische Chemische Gesellschaft, September 20, 22, 2022, Vienna, Austria. 2022;:90-90. https://hdl.handle.net/21.15107/rcub_cherry_5865 .
Petrović, Tamara, Gligorijević, Nevenka, Belaj, Ferdinand, Grgurić-Šipka, Sanja, Nikolić, Stefan, Krstić, Milena, Poljarević, Jelena, Mihajlović-Lalić, Ljiljana, "PO-017 Oxorhenium(V) complexes in the drug combination study" in Österreichische Chemische Gesellschaft, September 20, 22, 2022, Vienna, Austria (2022):90-90, https://hdl.handle.net/21.15107/rcub_cherry_5865 .