Synthesis of novel urea and sulfonamide derivatives of isatin schiff bases as potential anti-cancer agents

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dc.authorid0000-0003-1796-4706en_US
dc.contributor.authorDemirel, Ural Ufuk
dc.contributor.authorÖlgen, Süreyya
dc.contributor.authorKaraman, Ecem Fatma
dc.contributor.authorTanol, Mehmet
dc.contributor.authorÖzden, Sibel
dc.contributor.authorGöker, Hakan
dc.date.accessioned2022-08-16T11:39:50Z
dc.date.available2022-08-16T11:39:50Z
dc.date.issued2022en_US
dc.departmentFakülteler, Eczacılık Meslek Bilimleri Bölümü, Farmasötik Kimya Ana Bilim Dalıen_US
dc.description.abstractBackground: 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 µM, respectively. They showed better inhibition potencies than the reference compound doxorubicin, and its value was measured as 51.15 μM in the same culture assay. The cytotoxic activities of the compounds in other cell lines were found to be less potent compared to doxoru-bicin. 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.en_US
dc.identifier.citationDemirel, U. U., Ölgen, S., Karaman, E. F., Tanol, M., Özden, S., Göker, H. (2022). Synthesis of novel urea and sulfonamide derivatives of isatin schiff bases as potential anti-cancer agents. Letters in Drug Design & Discovery, 19(9), 847-857.en_US
dc.identifier.endpage857en_US
dc.identifier.issn1570-1808
dc.identifier.issue9en_US
dc.identifier.scopus2-s2.0-85134942567
dc.identifier.scopusqualityQ3
dc.identifier.startpage847en_US
dc.identifier.urihttps://hdl.handle.net/20.500.12939/2898
dc.identifier.volume19en_US
dc.identifier.wosWOS:000847327000008
dc.identifier.wosqualityN/A
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.institutionauthorDemirel, Ural Ufuk
dc.language.isoen
dc.publisherBentham Science Publishersen_US
dc.relation.ispartofLetters in Drug Design and Discovery
dc.relation.isversionof10.2174/1570180819666220224115908en_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectADME Predictionen_US
dc.subjectCytotoxicityen_US
dc.subjectIsatinen_US
dc.subjectMolecular Dockingen_US
dc.subjectSchiff Basesen_US
dc.subjectSynthesisen_US
dc.subjectUrea And Sulfonamide Derivativesen_US
dc.titleSynthesis of novel urea and sulfonamide derivatives of isatin schiff bases as potential anti-cancer agents
dc.typeArticle

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