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Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors.

Bioorg Med Chem Lett; 20(9): 2998-3002, 2010 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-20382527
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.