6127-11-3Relevant articles and documents
Discovery of GNF-5837, a selective TRK inhibitor with efficacy in rodent cancer tumor models
Albaugh, Pam,Fan, Yi,Mi, Yuan,Sun, Fangxian,Adrian, Francisco,Li, Nanxin,Jia, Yong,Sarkisova, Yelena,Kreusch, Andreas,Hood, Tami,Lu, Min,Liu, Guoxun,Huang, Shenlin,Liu, Zuosheng,Loren, Jon,Tuntland, Tove,Karanewsky, Donald S.,Seidel, H. Martin,Molteni, Valentina
supporting information; experimental part, p. 140 - 145 (2012/04/10)
Neurotrophins and their receptors (TRKs) play key roles in the development of the nervous system and the maintenance of the neural network. Accumulating evidence points to their role in malignant transformations, chemotaxis, metastasis, and survival signaling and may contribute to the pathogenesis of a variety of tumors of both neural and non-neural origin. By screening the GNF kinase collection, a series of novel oxindole inhibitors of TRKs were identified. Optimization led to the identification of GNF-5837 (22), a potent, selective, and orally bioavailable pan-TRK inhibitor that inhibited tumor growth in a mouse xenograft model derived from RIE cells expressing both TRKA and NGF. The properties of 22 make it a good tool for the elucidation of TRK biology in cancer and other nononcology indications.
New substituted spiro[cycloalkyl-1,3'-indo]-2'(1'H)-one derivatives and their use as p38 mitogen-activated kinase inhibitors
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Page/Page column 29, (2009/10/21)
This invention is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy.
COMPOUNDS AND COMPOSITIONS AS KINASE INHIBITORS
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Page/Page column 27-28, (2008/12/06)
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