Synthesis, Characterization, and Investigation of Anti-Inflammatory and Cytotoxic Activities of Novel Thiourea Derivatives of Naproxen.

Autor: Nedeljković N; Department of Pharmacy, Faculty of Medical Sciences, University of Kragujevac, Svetozara Markovića 69, 34000 Kragujevac, Serbia., Nikolić M; Department of Pharmacy, Faculty of Medical Sciences, University of Kragujevac, Svetozara Markovića 69, 34000 Kragujevac, Serbia., Čanović P; Department of Biochemistry, Faculty of Medical Sciences, University of Kragujevac, Svetozara Markovića 69, 34000 Kragujevac, Serbia., Zarić M; Department of Biochemistry, Faculty of Medical Sciences, University of Kragujevac, Svetozara Markovića 69, 34000 Kragujevac, Serbia., Živković Zarić R; Department of Pharmacology and Toxicology, Faculty of Medical Sciences, University of Kragujevac, Svetozara Markovića 69, 34000 Kragujevac, Serbia., Bošković J; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia., Vesović M; Department of Pharmacy, Faculty of Medical Sciences, University of Kragujevac, Svetozara Markovića 69, 34000 Kragujevac, Serbia., Bradić J; Department of Pharmacy, Faculty of Medical Sciences, University of Kragujevac, Svetozara Markovića 69, 34000 Kragujevac, Serbia.; Center of Excellence for Redox Balance Research in Cardiovascular and Metabolic Disorders, Svetozara Markovića 69, 34000 Kragujevac, Serbia., Anđić M; Department of Pharmacy, Faculty of Medical Sciences, University of Kragujevac, Svetozara Markovića 69, 34000 Kragujevac, Serbia.; Center of Excellence for Redox Balance Research in Cardiovascular and Metabolic Disorders, Svetozara Markovića 69, 34000 Kragujevac, Serbia., Kočović A; Department of Pharmacy, Faculty of Medical Sciences, University of Kragujevac, Svetozara Markovića 69, 34000 Kragujevac, Serbia.; Center of Excellence for Redox Balance Research in Cardiovascular and Metabolic Disorders, Svetozara Markovića 69, 34000 Kragujevac, Serbia., Nikolić M; Center of Excellence for Redox Balance Research in Cardiovascular and Metabolic Disorders, Svetozara Markovića 69, 34000 Kragujevac, Serbia.; Department of Physiology, Faculty of Medical Sciences, University of Kragujevac, Svetozara Markovića 69, 34000 Kragujevac, Serbia., Jakovljević V; Center of Excellence for Redox Balance Research in Cardiovascular and Metabolic Disorders, Svetozara Markovića 69, 34000 Kragujevac, Serbia.; Department of Physiology, Faculty of Medical Sciences, University of Kragujevac, Svetozara Markovića 69, 34000 Kragujevac, Serbia.; Department of Human Pathology, First Moscow State Medical University IM Sechenov, 119435 Moscow, Russia., Vujić Z; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia., Dobričić V; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia.
Jazyk: angličtina
Zdroj: Pharmaceutics [Pharmaceutics] 2023 Dec 19; Vol. 16 (1). Date of Electronic Publication: 2023 Dec 19.
DOI: 10.3390/pharmaceutics16010001
Abstrakt: The objective of this study was to synthesize seven novel thiourea derivatives of naproxen ( 8 - 14 ), examine the anti-inflammatory activity of the newly synthesized compounds, investigate the cytotoxic potential of both sets of synthesized compounds ( 1 - 7 and 8 - 14 ), and select the most promising anti-inflammatory and antitumor drug candidates. The results of the in vivo anti-inflammatory study clearly showed that compounds 8 and 9 were capable of decreasing paw edema, as evident from a high percentage of inhibition (44.83% and 49.29%, respectively). In addition, the results of in vitro enzyme inhibition assays demonstrated that neither of the newly synthesized compounds reached 50% inhibition of 5-LOX at concentrations lower than 100 µM. In terms of antitumor potential, derivatives 3 and 8 exhibited strong cytotoxic effects on the HeLa cell line, suggesting the involvement of the extrinsic pathway of apoptosis. According to the overall results obtained for both sets of synthesized molecules, derivatives 4 and 8 can be underlined as molecules with the strongest anti-inflammatory activity, while derivatives 3 and 8 are the most promising cytotoxic agents.
Databáze: MEDLINE
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