Synthesis, Characterization, and Investigation of Anti-Inflammatory and Cytotoxic Activities of Novel Thiourea Derivatives of Naproxen
Аутори
Nedeljković, NikolaNikolić, Miloš
Čanović, Petar
Zarić, Milan
Živković-Zarić, Radica
Bošković, Jelena
Vesović, Marina
Bradić, Jovana
Anđić, Marijana
Kočović, Aleksandar
Nikolić, Marina
Jakovljević, Vladimir
Vujić, Zorica
Dobričić, Vladimir
Чланак у часопису (Објављена верзија)
Метаподаци
Приказ свих података о документуАпстракт
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 molecul...es, 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.
Кључне речи:
naproxen / thiourea / anti-inflammatory activity / paw edema / cytotoxic activity / MTT / apoptosis / COX-2 / 5-LOXИзвор:
Pharmaceutics, 2024, 16, 1, 1-Издавач:
- MDPI
Финансирање / пројекти:
- InfCanPlay - Utilization of interplay between inflammation and cancer in the development of compounds with anticancer activity (RS-ScienceFundRS-Ideje-7739840)
- Министарство науке, технолошког развоја и иновација Републике Србије, институционално финансирање - 200161 (Универзитет у Београду, Фармацеутски факултет) (RS-MESTD-inst-2020-200161)
- Министарство науке, технолошког развоја и иновација Републике Србије, институционално финансирање - 200111 (Универзитет у Крагујевцу, Медицински факултет) (RS-MESTD-inst-2020-200111)
- Faculty of Medical Sciences, University of Kragujevac (Junior Project 11/20)
DOI: 10.3390/pharmaceutics16010001
ISSN: 1999-4923
PubMed: 38276479
WoS: 001151136100001
Scopus: 2-s2.0-85183122869
Институција/група
PharmacyTY - JOUR AU - Nedeljković, Nikola AU - Nikolić, Miloš AU - Čanović, Petar AU - Zarić, Milan AU - Živković-Zarić, Radica AU - Bošković, Jelena AU - Vesović, Marina AU - Bradić, Jovana AU - Anđić, Marijana AU - Kočović, Aleksandar AU - Nikolić, Marina AU - Jakovljević, Vladimir AU - Vujić, Zorica AU - Dobričić, Vladimir PY - 2024 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/5449 AB - 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. PB - MDPI T2 - Pharmaceutics T1 - Synthesis, Characterization, and Investigation of Anti-Inflammatory and Cytotoxic Activities of Novel Thiourea Derivatives of Naproxen VL - 16 IS - 1 SP - 1 DO - 10.3390/pharmaceutics16010001 ER -
@article{ author = "Nedeljković, Nikola and Nikolić, Miloš and Čanović, Petar and Zarić, Milan and Živković-Zarić, Radica and Bošković, Jelena and Vesović, Marina and Bradić, Jovana and Anđić, Marijana and Kočović, Aleksandar and Nikolić, Marina and Jakovljević, Vladimir and Vujić, Zorica and Dobričić, Vladimir", year = "2024", abstract = "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.", publisher = "MDPI", journal = "Pharmaceutics", title = "Synthesis, Characterization, and Investigation of Anti-Inflammatory and Cytotoxic Activities of Novel Thiourea Derivatives of Naproxen", volume = "16", number = "1", pages = "1", doi = "10.3390/pharmaceutics16010001" }
Nedeljković, N., Nikolić, M., Čanović, P., Zarić, M., Živković-Zarić, R., Bošković, J., Vesović, M., Bradić, J., Anđić, M., Kočović, A., Nikolić, M., Jakovljević, V., Vujić, Z.,& Dobričić, V.. (2024). Synthesis, Characterization, and Investigation of Anti-Inflammatory and Cytotoxic Activities of Novel Thiourea Derivatives of Naproxen. in Pharmaceutics MDPI., 16(1), 1. https://doi.org/10.3390/pharmaceutics16010001
Nedeljković N, Nikolić M, Čanović P, Zarić M, Živković-Zarić R, Bošković J, Vesović M, Bradić J, Anđić M, Kočović A, Nikolić M, Jakovljević V, Vujić Z, Dobričić V. Synthesis, Characterization, and Investigation of Anti-Inflammatory and Cytotoxic Activities of Novel Thiourea Derivatives of Naproxen. in Pharmaceutics. 2024;16(1):1. doi:10.3390/pharmaceutics16010001 .
Nedeljković, Nikola, Nikolić, Miloš, Čanović, Petar, Zarić, Milan, Živković-Zarić, Radica, Bošković, Jelena, Vesović, Marina, Bradić, Jovana, Anđić, Marijana, Kočović, Aleksandar, Nikolić, Marina, Jakovljević, Vladimir, Vujić, Zorica, Dobričić, Vladimir, "Synthesis, Characterization, and Investigation of Anti-Inflammatory and Cytotoxic Activities of Novel Thiourea Derivatives of Naproxen" in Pharmaceutics, 16, no. 1 (2024):1, https://doi.org/10.3390/pharmaceutics16010001 . .