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Novel imidazo[2,1-b]thiazole-based anticancer agents as potential focal adhesion kinase inhibitors: Synthesis, in silico and in vitro evaluation.
Basoglu, Faika; Ulusoy-Güzeldemirci, Nuray; Akalin-Çiftçi, Gülsen; Çetinkaya, Serap; Ece, Abdulilah.
Afiliação
  • Basoglu F; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Istanbul University, Istanbul, Turkey.
  • Ulusoy-Güzeldemirci N; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, European University of Lefke, Northern Cyprus, Turkey.
  • Akalin-Çiftçi G; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Istanbul University, Istanbul, Turkey.
  • Çetinkaya S; Department of Biochemistry, Faculty of Pharmacy, Anadolu University, Eskisehir, Turkey.
  • Ece A; Department of Molecular Biology and Genetics, Science Faculty, Sivas Cumhuriyet University, Sivas, Turkey.
Chem Biol Drug Des ; 98(2): 270-282, 2021 08.
Article em En | MEDLINE | ID: mdl-34021971
The 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.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Tiazóis / Inibidores de Proteínas Quinases / Proteína-Tirosina Quinases de Adesão Focal / Imidazóis / Antineoplásicos Limite: Humans Idioma: En Revista: Chem Biol Drug Des Ano de publicação: 2021 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Tiazóis / Inibidores de Proteínas Quinases / Proteína-Tirosina Quinases de Adesão Focal / Imidazóis / Antineoplásicos Limite: Humans Idioma: En Revista: Chem Biol Drug Des Ano de publicação: 2021 Tipo de documento: Article