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Synthesis, Cytotoxicity Assessment, and Molecular Docking of 4-Substituted-2-p-tolylthiazole Derivatives as Probable c-Src and erb Tyrosine Kinase Inhibitors

机译:作为可能的c-Src和erb酪氨酸激酶抑制剂的4-取代-2-对甲苯噻唑衍生物的合成,细胞毒性评估和分子对接

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摘要

In the current project we focused on the synthesis of 4-Substituted-2-p-tolylthiazole derivatives. Cytotoxicity of synthesized compounds were evaluated against T47D breast cancer cell line and also all of the final compounds 3−7 were docked into the active site of c-Src and erb tyrosine kinases. Compound 4 was the most potent derivative in cytotoxicity assay (IC50 = 2.5 µg/mL) and it was also the most potent inhibitor of erb tyrosine kinase (Binding free energy: −10.18 kcal/mol).(doi: 10.5562/cca1939)
机译:在当前的项目中,我们专注于4-取代-2-对甲苯噻唑衍生物的合成。评估了合成的化合物对T47D乳腺癌细胞系的细胞毒性,并且所有最终化合物3-7都被插入c-Src和erb酪氨酸激酶的活性位点。化合物4是细胞毒性测定中最有效的衍生物(IC50 = 2.5 µg / mL),也是最有效的erb酪氨酸激酶抑制剂(结合自由能:−10.18 kcal / mol)。(doi:10.5562 / cca1939)

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