Sürdürülebilir Kalkınma Amaçları

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• MakaleAçık Erişim2023/r/kostu/10957
  Benzimidazole-thiazole hybrids; synthesis, structure elucidation and cytotoxic properties

  Cevik, Ozge; Erdoğan, Ömer; Şahin, Zafer; Demirayak, Şeref; Coşkun, Göknil Pelin

  Objective: Neuroblastoma is one of the leading tumors among the childhood cancers and the treatment of the disease is currently being investigated. As the metastatic ability of the cells is high, current anticancer therapy needs improvement. Methods: Therefore, here five novel benzimidazole-thiazole compounds were synthesized. Their structures were elucidated using spectroscopic methods like FTIR, NMR and Mass analysis. The synthesis monitoring and purity of the compounds were performed with chromatographic methods. The compounds biological activity on SH-SY5Y neuroblastoma cell line was investigated using MTT assay. Results: All of the tested compounds showed moderate cytotoxic activity. The best IC50 was obtained from compound 6b with the IC50 value of 175,02±4,17 µM. Conclusion: These results indicated that benzimidazole-thiazole core is important for anti neuroblastoma activity, however, the ability of intramolecular hydrogen bonding could block the anticancer activity

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• MakaleAçık Erişim2023Scopus SJRQ1/r/kostu/10253
  Discovery of Novel Thiophene/Hydrazones: In Vitro and In Silico Studies against Pancreatic Cancer

  Coskun, Goknil Pelin; Ozhan, Yagmur; Dobričić, Vladimir; Bošković, Jelena; Reis, Rengin; Sipahi, Hande; Sahin, Zafer; Demirayak, Seref

  Cancer is the disease with the highest mortality. Drug studies contribute to promising treatments; however there is an urgent need for selective drug candidates. Pancreatic cancer is difficult to treat and the cancer progresses rapidly. Unfortunately, current treatments are ineffective. In this study, ten new diarylthiophene-2-carbohydrazide derivatives were synthesized and evaluated for their pharmacological activity. The 2D and 3D anticancer activity studies suggested the compounds 7a, 7d, and 7f were promising. Among these, 7f (4.86 µM) showed the best 2D inhibitory activity against PaCa-2 cells. Compounds 7a, 7d and 7f were also tested for their cytotoxic effects on healthy cell line but only compound 7d showed selectivity. Compounds 7a, 7d, and 7f showed the best 3D cell line inhibitory effect according to spheroid diameters. The compounds were screened for their COX-2 and 5-LOX inhibitory activity. For COX-2, the best IC50 value was observed for 7c (10.13 µM) and all compounds showed significantly lower inhibition compared to standard. In the 5-LOX inhibition study, compounds 7a (3.78 µM), 7c (2.60 µM), 7e (3.3 µM), and 7f (2.94 µM) demonstrated influential activity compared to standard. Regarding molecular docking studies, binding mode of compounds 7c, 7e, and 7f to the 5-LOX enzyme were non-redox or redox types, but not the iron-binding type. As dual inhibitors of 5-LOX and pancreatic cancer cell line, 7a and 7f were identified as the most promising compounds.

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  AtıfScopus7·WoS7·OpenAlex6

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