1229038-76-9Relevant academic research and scientific papers
Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors
Williams, David K.,Chen, Xiao-Tao,Tarby, Christine,Kaltenbach, Robert,Cai, Zhen-Wei,Tokarski, John S.,An, Yongmi,Sack, John S.,Wautlet, Barri,Gullo-Brown, Johnni,Henley, Benjamin J.,Jeyaseelan, Robert,Kellar, Kristen,Manne, Veeraswamy,Trainor, George L.,Lombardo, Louis J.,Fargnoli, Joseph,Borzilleri, Robert M.
, p. 2998 - 3002 (2010)
Biarylamine-based inhibitors of Met kinase have been identified. Lead compounds demonstrate nanomolar potency in Met kinase biochemical assays and significant activity in the Met-driven GTL-16 human gastric carcinoma cell line. X-ray crystallography revealed that these compounds adopt a bioactive conformation, in the kinase domain, consistent with that previously seen with 2-pyridone-based Met kinase inhibitors. Compound 9b demonstrated potent in vivo antitumor activity in the GTL-16 human tumor xenograft model.
