WoS İndeksli Yayınlar Koleksiyonu

Permanent URI for this collectionhttps://hdl.handle.net/20.500.12514/3595

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Eco-Friendly Synthesis of Thiazole Derivatives Using Recyclable Cross-Linked Chitosan Hydrogel Biocatalyst Under Ultrasonic Irradiation as Anti-Hepatocarcinogenic Agents
(Mdpi, 2024) Gomha, Sobhi M.; Abd El-Ghany, Nahed A.; Ebaid, Manal S.; Abolibda, Tariq Z.; E. A. Zaki, Magdi; Alhilal, Mohammad; Mohamed, Nadia A.
In the current study, pyromellitimide benzoyl thiourea cross-linked chitosan (PIBTU-CS) hydrogel, was evaluated as a green biocatalyst for the efficient synthesis of novel thiazole derivatives. The PIBTU-CS hydrogel showcased key advantages, such as an expanded surface area and superior thermal stability, establishing it as a potent eco-friendly catalyst. By employing PIBTU-CS alongside ultrasonic irradiation, we successfully synthesized a series of novel thiazoles through the reaction of 2-(4-((2-carbamothioylhydrazineylidene)methyl)phenoxy)-N-(4-chlorophenyl)acetamide with a variety of hydrazonoyl halides (6a-f) and alpha-haloketones (8a-c or 10a,b). A comparative analysis with TEA revealed that PIBTU-CS hydrogel consistently delivered significantly higher yields. This synthetic strategy provided several benefits, including mild reaction conditions, reduced reaction times, and consistently high yields. The robustness of PIBTU-CS was further underscored by its ability to be reused multiple times without a substantial reduction in catalytic efficiency. The structures of the synthesized thiazole derivatives were meticulously characterized using a range of analytical techniques, including IR, 1H-NMR, 13C-NMR, and mass spectrometry (MS), confirming their successful formation. These results underscore the potential of PIBTU-CS hydrogel as a sustainable and recyclable catalyst for the synthesis of heterocyclic compounds. Additionally, all synthesized products were tested for their anticancer activity against HepG2-1 cells, with several new compounds exhibiting good anticancer effects.
Novel thiadiazole-thiazole hybrids: synthesis, molecular docking, and cytotoxicity evaluation against liver cancer cell lines
(Taylor & Francis Online, 2022) Aljohani, Ghadah F.; Abolibda, Tariq Z.; Alhilal, Mohammad; Al-Humaidi, Jehan Y.; Alhilal, Suzan; Ahmed, Hoda A.; Gomha, Sobhi M.
One of the worst diseases, cancer claims millions of lives each year throughout the world, necessitating the creation of novel treatments. In this study, we designed a novel series of 1,3,4-thiadiazoles through the reaction of 2-(4-methyl-2-(2-(1-phenylethylidene)hydrazineyl)thiazole-5-carbonyl)-N-phenylhydrazine-1-carbothioamide (3) with the proper hydrazonoyl halides. Using the MTT assay, the newly synthesized thiadiazoles' growth-inhibitory potential against the liver cancer cell line HepG2-1 was assessed. In comparison to the standard drug doxorubicin (IC50 = 0.72 ± 0.52 µM), the results showed that two compounds, 16b and 21 (IC50 = 0.69 ± 0.41 and 1.82 ± 0.94 µM, respectively) had promising anticancer activity. The structural activity relationship (SAR) was investigated. In addition, molecular docking analysis onto quinone oxidoreductase2 (NQO2) receptor (PDB: 4ZVM) was investigated against the potent compounds to examine the reliability of the in vitro results. The newly prepared thiadiazole-thiazole hybrids are therefore regarded as potent anticancer drugs.

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Browsing WoS İndeksli Yayınlar Koleksiyonu by Author "Abolibda, Tariq Z."