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Page 1
Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells.
Henry JR, Kaufman MD, Peng SB, Ahn YM, Caldwell TM, Vogeti L, Telikepalli H, Lu WP, Hood MM, Rutkoski TJ, Smith BD, Vogeti S, Miller D, Wise SC, Chun L, Zhang X, Zhang Y, Kays L, Hipskind PA, Wrobleski AD, Lobb KL, Clay JM, Cohen JD, Walgren JL, McCann D, Patel P, Clawson DK, Guo S, Manglicmot D, Groshong C, Logan C, Starling JJ, Flynn DL. Henry JR, et al. Among authors: wrobleski ad. J Med Chem. 2015 May 28;58(10):4165-79. doi: 10.1021/acs.jmedchem.5b00067. Epub 2015 May 12. J Med Chem. 2015. PMID: 25965804
Identification of LY3522348: A Highly Selective and Orally Efficacious Ketohexokinase Inhibitor.
Durham TB, Hao J, Spinazze P, Stack DR, Toth JL, Massey S, Mbofana CT, Johnston RD, Lineswala JP, Wrobleski A, Mínguez JM, Perez C, Smith DL, Lamar J, Leon R, Corkins C, Durbin J, Tung F, Guo S, Linder RJ, Yumibe N, Wang W, MacKrell J, Antonellis M, Mascaro B. Durham TB, et al. J Med Chem. 2023 Dec 14;66(23):15960-15976. doi: 10.1021/acs.jmedchem.3c01410. Epub 2023 Nov 22. J Med Chem. 2023. PMID: 37992274
Facile C-N cleavage in a series of bridged lactams.
Lei Y, Wrobleski AD, Golden JE, Powell DR, Aubé J. Lei Y, et al. Among authors: wrobleski ad. J Am Chem Soc. 2005 Apr 6;127(13):4552-3. doi: 10.1021/ja050214m. J Am Chem Soc. 2005. PMID: 15796502