Novel imidazo[2,1-b]thiazole-based anticancer agents as potential focal adhesion kinase inhibitors: Synthesis, in silico and in vitro evaluation

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dc.authoridEce, Abdulilah/0000-0002-3087-5145
dc.authoridBasoglu, Faika/0000-0002-4890-3124
dc.contributor.authorBasoglu, Faika
dc.contributor.authorUlusoy-Guzeldemirci, Nuray
dc.contributor.authorAkalin-Ciftci, Gulsen
dc.contributor.authorCetinkaya, Serap
dc.contributor.authorEce, Abdulilah
dc.date.accessioned2024-10-26T18:11:04Z
dc.date.available2024-10-26T18:11:04Z
dc.date.issued2021
dc.departmentSivas Cumhuriyet Üniversitesi
dc.description.abstractThe purpose of this study was to synthesize imidazo[2,1-b]thiazole derivatives, characterize them with spectroscopical techniques and investigate for cytotoxic and apoptotic effects on glioma C6 cancer cell line. The in vitro anticancer activities were also investigated against focal adhesion kinase. Most of the compounds, particularly the derivatives carrying 3-oxo-1-tiya-4-azaspiro[4.5]decane moiety, exhibited higher or comparable activities in comparison with the reference drug, cisplatin. Compounds with methyl, propyl, phenyl moieties at the eighth and second position of the spirothiazolidinone ring showed high FAK inhibitory activities. In addition, molecular docking studies shed light on the binding modes of the synthesized compounds. The critical interactions with amino acid residues located in the active site were revealed. The results obtained from both biological assay data and computational results might provide insight into developing new inhibitors against focal adhesion kinase.
dc.description.sponsorshipIstanbul Universitesi
dc.description.sponsorshipIstanbul Universitesi
dc.identifier.doi10.1111/cbdd.13896
dc.identifier.endpage282
dc.identifier.issn1747-0277
dc.identifier.issn1747-0285
dc.identifier.issue2
dc.identifier.pmid34021971
dc.identifier.scopus2-s2.0-85107821211
dc.identifier.scopusqualityQ2
dc.identifier.startpage270
dc.identifier.urihttps://doi.org/10.1111/cbdd.13896
dc.identifier.urihttps://hdl.handle.net/20.500.12418/30488
dc.identifier.volume98
dc.identifier.wosWOS:000660776200001
dc.identifier.wosqualityQ3
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherWiley
dc.relation.ispartofChemical Biology & Drug Design
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectfocal adhesion kinase
dc.subjectImidazo[2
dc.subject1-b]thiazole
dc.subjectmolecular docking
dc.titleNovel imidazo[2,1-b]thiazole-based anticancer agents as potential focal adhesion kinase inhibitors: Synthesis, in silico and in vitro evaluation
dc.typeArticle

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