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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
Author(s) -
Başoğlu Faika,
UlusoyGüzeldemirci Nuray,
AkalınÇiftçi Gülşen,
Çetinkaya Serap,
Ece Abdulilah
Publication year - 2021
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.13896
Subject(s) - thiazole , chemistry , focal adhesion , moiety , in vitro , stereochemistry , in silico , docking (animal) , kinase , cisplatin , lead compound , biochemistry , signal transduction , biology , medicine , genetics , nursing , chemotherapy , gene
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.