N-(3-Substituted-benzylidene-2-oxoindolin-5-yl) acetamide Derivatives as Src Kinase Inhibitors: Synthesis, Biological Evaluation and Molecular Docking Studies

The synthesis of new N-(3-substituted-benzylidene-2-oxoindolin-5-yl) acetamide (5-14) derivatives along with their inhibitory activity against Src is reported. Among all compounds, only 10, 12 and 13 were found slightly active against Src with IC50 values of 3.55, 6.39 and 7.29 mM, respectively. Docking studies have been also performed to analyze the binding mode of compounds and the results showed that the most active compound 10 showed a hydrogen bond with Leu273 for the binding to the Src active site. It was found that replacement of ethylthiourea, benzylthiourea and methylaminosulphonic acid group with acetamido group decreases the activity of compounds.