Synthesis and anti-tyrosine kinase activity of 3-(substituted-benzylidene)-1, 3-dihydro-indolin derivatives: investigation of their role against p60c-Src receptor tyrosine kinase with the application of receptor docking studies

Synthesis and Biological Evaluation of 3-(Substituted-benzylidene)-1,3-dihydro-indolin Derivatives as Human Protein Kinase CK2 and p60c-Src Tyrosine Kinase Inhibitors

“…The synthesis and analysis data of compound 7 were reported in this paper and compound 9 was reported in our previous publication. 23) Data on other 3-(substituted-benzylidene)-1,3-dihydro-indolin-2-one derivatives were previously reported by Daisley and Walker 34) (compound 3), Neber and Rocker 35) (4 and 6), Howard et al 36) (5), and Sun et al 26) (compound 8). An assay for inhibitor testing was set up in analogy to Yim et al 15) and Sarno et al 16) with modifications as described in Materials and Methods.…”

“…Although knovenagel reaction was reported for the synthesis of 3-(substituted-benzylidene)-1,3-dihydro-indolin-2-one derivatives, it was successfully applied for the synthesis of 3-(substituted-benzylidene)-1,3-dihydro indolin-2-thione derivatives in our laboratory. 23) Synthesis of oxoindole (1) was achieved by a Wolff-Kishner-like reduction of isatin with hydrazine hydrate.…”

“…22) In our previous study, several 3-(substituted-benzylidene)-1,3-dihydro-indolin-2-one and thione derivatives were reported as p60 c-Src protein tyrosine kinase inhibitors. 23) As the part of our interest in the area of protein kinase inhibitors, we synthesized four new 3-(substituted-benzylidene)-1,3-dihydro-indolin-2-one and thione derivatives. , a Claudia GÖTZ, b and Joachim JOSE benzylidene)-1,3-dihydro-indolin-2-one and thione derivatives 23) were tested for their inhibitory activity towards human recombinant protein kinase CK2.…”

“…23) As the part of our interest in the area of protein kinase inhibitors, we synthesized four new 3-(substituted-benzylidene)-1,3-dihydro-indolin-2-one and thione derivatives. , a Claudia GÖTZ, b and Joachim JOSE benzylidene)-1,3-dihydro-indolin-2-one and thione derivatives 23) were tested for their inhibitory activity towards human recombinant protein kinase CK2. Our results indicate that substituted 3-benzylidene-1,3-dihydro-indolin-2-thiones could provide a new molecular scaffold for the rational design of selective human CK2 inhibitors.…”

Synthesis and Antioxidant Properties of Novel N‐H and N‐Substituted Propanamide Derivatives

“…1) have radical scavenger effects and they may be considered as an effective source for combating oxidative damage [13]. These compounds have been previously reported in the literature as inhibitors of protein kinase [14]. The findings about 3-(substituted-benzylidene)-1,3-dihydroindolin-2-one and thione derivatives suggested that there is strong evidence between the tyrosine kinase inhibition and antioxidant activity.…”