Academic Journal
Synthesis of novel urea and sulfonamide derivatives of isatin schiff bases as potential anti - cancer agents
| العنوان: | Synthesis of novel urea and sulfonamide derivatives of isatin schiff bases as potential anti - cancer agents |
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| المؤلفون: | Demirel, Ural Ufuk, Ölgen, Süreyya, Karaman, Ecem Fatma, Tanol, Mehmet, Özden, Sibel, Göker, Hakan |
| المساهمون: | Eczacılık Fakültesi |
| بيانات النشر: | Bentham Science Publishers |
| سنة النشر: | 2022 |
| المجموعة: | Biruni University Institutional Repository (DSpace@Biruni) |
| مصطلحات موضوعية: | Urea and Sulfonamide Derivatives, Isatin, Schiff Bases, Cytotoxicity, Adme Prediction, Synthesis, Molecular Docking |
| الوصف: | Background: Among the many types of chemical scaffolds, isatin derivatives, including their Schiff bases, have been extensively studied to find novel therapeutic agents against cancer. Amide or urea groups containing derivatives were also discovered to be tyrosine kinase inhibitors. Objective: This study aims to find potent compounds by designing 16 novel urea and sulfonamide derivatives of isatin Schiff bases. Methods: Compounds were tested against PC-3, HepG2, SH-SY5Y, A549 cancerous, and NIH/3T3 non-cancerous cell lines using cell culture assay. Results: Among the tested compounds 7a, 7b, 7c, 7d, 7h, 8a, and 8f presented potential inhibitions against cellular proliferation activities of HepG2 cells with average IC50 values of 31.97, 42.13, 31.50, 47.98, 32.59, 43.44, and 37.81 mu M, respectively. They showed better inhibition potencies than the reference compound doxorubicin, and its value was measured as 51.15 mu M in the same culture assay. The cytotoxic activities of the compounds in other cell lines were found to be less potent compared to doxorubicin. Conclusion: In vitro experiments demonstrated that designed compounds have the first evidence that they might be active against hepatocellular carcinoma. According to ADME prediction results, all compounds presented drug-like and good metabolic properties. |
| نوع الوثيقة: | article in journal/newspaper |
| اللغة: | English |
| تدمد: | 1570-1808 1875-628X |
| Relation: | https://doi.org/0.2174/1570180819666220224115908; Letters in Drug Design & Discovery; Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı; https://hdl.handle.net/20.500.12445/2313; 19; 847; 857 |
| الاتاحة: | https://hdl.handle.net/20.500.12445/2313 https://doi.org/0.2174/1570180819666220224115908 |
| Rights: | info:eu-repo/semantics/openAccess |
| رقم الانضمام: | edsbas.CD44301E |
| قاعدة البيانات: | BASE |
| تدمد: | 15701808 1875628X |
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