Some novel 5-benzylidenethiazolo[3,2-b]-1,2,4-triazole-6(5H)-one derivatives in the battle against cancer: Design, synthesis and their biological activities

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dc.authorscopusidNazlıhan Aztopal / 55853882900
dc.authorscopusidEngin Ulukaya / 6602927353
dc.authorwosidNazlıhan Aztopal / MEQ-4752-2025
dc.authorwosidEngin Ulukaya / KYY-4020-2024
dc.contributor.authorAvcı, Ahmet
dc.contributor.authorAztopal, Nazlıhan
dc.contributor.authorGökhan Kelekçi, Nesrin
dc.contributor.authorUlukaya, Engin
dc.contributor.authorTozkoparan, Birsen
dc.date.accessioned2025-04-18T09:21:41Z
dc.date.available2025-04-18T09:21:41Z
dc.date.issued2025
dc.departmentİstinye Üniversitesi, Tıp Fakültesi, Temel Tıp Bilimleri Bölümü
dc.description.abstractConsidering the significant biological potential and the privileged status of the 1,2,4-triazole-5-thione scaffold as one of the essential building blocks in medicinal chemistry, a novel series of 30 new hybrid compounds of 1,2,4-triazole and 5-benzylidenethiazolidinone ring systems, named 5-benzilidene-thiazolo[3,2-b][1,2,4]triazole-6(5H)-one, were designed and synthesized in an attempt to obtain antiproliferative agents and EGFR inhibitors. Synthesized thiazolo[3,2-b][1,2,4]triazole-6(5H)-ones were investigated for their potential cytotoxic properties by cell viability, cell cycle, and cell death analyses. Compounds that exhibited more selective anti-growth activity in A549 cells were further scrutinized, revealing an accumulation in the G1 phase. Notably, compound 6e demonstrated outstanding results and was found to induce apoptosis. Molecular docking studies indicated that the designed compounds could act as EGFR inhibitors. Indeed, compounds 6i and 6j inhibited cell growth prevented EGFR-specific phosphorylation, and thus downregulated EGFR signaling, and inhibited EGFR enzyme activity with IC50 values of 2.46 μM and 4.72 μM, respectively. Additionally, druglikeness and some pharmaceutical properties of the synthesized compounds were predicted. This study underscores the promising therapeutic potential of the novel thiazolo[3,2-b]-1,2,4-triazole derivatives as EGFR inhibitors. © 2024 Elsevier B.V.
dc.description.sponsorshipThis research has received funding from the Hacettepe University Scientific Research Projects Coordination Unit (Project No: TYL-2018-17558) and and the Scientific and Technological Research Council of Turkey (T\u00DCB\u0130TAK) (Project No: 119S854), Ankara, Turkey.
dc.identifier.citationAvci, A., Aztopal, N., Gökhan-Kelekçi, N., Ulukaya, E., & Tozkoparan, B. (2025). Some novel 5-benzylidenethiazolo [3, 2-b]-1, 2, 4-triazole-6 (5H)-one derivatives in the battle against cancer: Design, synthesis and their biological activities. Journal of Molecular Structure, 1327, 141169.
dc.identifier.doi10.1016/j.molstruc.2024.141169
dc.identifier.issn00222860
dc.identifier.scopus2-s2.0-85214197776
dc.identifier.scopusqualityQ1
dc.identifier.urihttp://dx.doi.org/10.1016/j.molstruc.2024.141169
dc.identifier.urihttps://hdl.handle.net/20.500.12713/6766
dc.identifier.volume1327
dc.indekslendigikaynakScopus
dc.institutionauthorAztopal, Nazlıhan
dc.institutionauthorUlukaya, Engin
dc.institutionauthoridNazlıhan Aztopal / 0000-0003-3118-8061
dc.institutionauthoridEngin Ulukaya / 0000-0003-4875-5472
dc.language.isoen
dc.publisherElsevier B.V.
dc.relation.ispartofJournal of Molecular Structure
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectAntiproliferative Activity
dc.subjectCytotoxic Activity
dc.subjectEGFR İnhibition Activity
dc.titleSome novel 5-benzylidenethiazolo[3,2-b]-1,2,4-triazole-6(5H)-one derivatives in the battle against cancer: Design, synthesis and their biological activities
dc.typeArticle

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