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Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for the treatment of cancer.
Cui JJ, McTigue M, Nambu M, Tran-Dubé M, Pairish M, Shen H, Jia L, Cheng H, Hoffman J, Le P, Jalaie M, Goetz GH, Ryan K, Grodsky N, Deng YL, Parker M, Timofeevski S, Murray BW, Yamazaki S, Aguirre S, Li Q, Zou H, Christensen J. Cui JJ, et al. J Med Chem. 2012 Sep 27;55(18):8091-109. doi: 10.1021/jm300967g. Epub 2012 Sep 10. J Med Chem. 2012. PMID: 22924734
A selective and oral small molecule inhibitor of vascular epithelial growth factor receptor (VEGFR)-2 and VEGFR-1 inhibits neovascularization and vascular permeability.
Patel N, Sun L, Moshinsky D, Chen H, Leahy KM, Le P, Moss KG, Wang X, Rice A, Tam D, Laird AD, Yu X, Zhang Q, Tang C, McMahon G, Howlett A. Patel N, et al. J Pharmacol Exp Ther. 2003 Sep;306(3):838-45. doi: 10.1124/jpet.103.052167. Epub 2003 May 23. J Pharmacol Exp Ther. 2003. PMID: 12766257
207 results