Croatica Chemica Acta, Vol. 86 No. 3, 2013.
Original scientific paper
https://doi.org/10.5562/cca1939
Synthesis, Cytotoxicity Assessment, and Molecular Docking of 4-Substituted-2-p-tolylthiazole Derivatives as Probable c-Src and erb Tyrosine Kinase Inhibitors
Alireza Aliabadi
; Department of Medicinal Chemistry, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran; Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Science
Alireza Foroumadi
; Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran 14174, Iran
Maliheh Safavi
; Institute of Biochemistry and Biophysics, Department of Biochemistry, University of Tehran, Tehran, Iran
Sussan K. Ardestani
; Institute of Biochemistry and Biophysics, Department of Biochemistry, University of Tehran, Tehran, Iran
Abstract
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)
Keywords
synthesis; phenylthiazole; cytotoxicity; breast cancer; tyrosine kinase; docking
Hrčak ID:
111219
URI
Publication date:
20.11.2013.
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