Novel Aminomethylindole Derivatives as Inhibitors of pp60(c-Src) Tyrosine Kinase: Synthesis and Biological Activity

摘要

The pp60(c-Src) is one of the ubiquitously expressed Src family kinases and has important functions in malignant cells, including regulation of cell division, growth factor signaling, and movement. Therefore, investigating new small molecule inhibitors of pp60(c-Src) is important to discover and develop novel therapeutics for cancer and metastasis. Moreover, some of the small molecule inhibitors that do not qualify for therapeutic use may become very useful tool to explore the role of Src kinase in normal cells as well as in a variety of disease models. Our continuous efforts to find novel inhibitors of pp60(c-Src) aimed for therapeutic and research use, we synthesized newly designed aminomethylindole derivatives as novel small molecule inhibitors and investigated their inhibitory effect on pp60(c-Src) tyrosine kinase. Here, we report one potential inhibitor of the pp60(c-Src) from five active molecules of all nine compounds, which were synthesized and screened for the biological activity of the molecules against pp60(c-Src) target.