التفاصيل البيبلوغرافية
| العنوان: |
Design, synthesis and structure–activity relationships of novel biarylamine-based Met kinase inhibitors |
| المؤلفون: |
Williams, David K. david.williams@bms.com, Chen, Xiao-Tao1, Tarby, Christine1, Kaltenbach, Robert1, Cai, Zhen-Wei1, Tokarski, John S.1, An, Yongmi1, Sack, John S.1, Wautlet, Barri1, Gullo-Brown, Johnni1, Henley, Benjamin J.1, Jeyaseelan, Robert1, Kellar, Kristen1, Manne, Veeraswamy1, Trainor, George L.1, Lombardo, Louis J.1, Fargnoli, Joseph1, Borzilleri, Robert M.1 |
| المصدر: |
Bioorganic & Medicinal Chemistry Letters. May2010, Vol. 20 Issue 9, p2998-3002. 5p. |
| مصطلحات موضوعية: |
*STRUCTURE-activity relationships, *X-ray crystallography, *ENZYME inhibitors, *ANTINEOPLASTIC agents, *HEPATOCYTE growth factor, *CHEMICAL synthesis, *ENZYMES, *CANCER cells |
| مستخلص: |
Abstract: 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. [Copyright &y& Elsevier] |
| قاعدة البيانات: |
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