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Page 1
Discovery of KIN-3248, An Irreversible, Next Generation FGFR Inhibitor for the Treatment of Advanced Tumors Harboring FGFR2 and/or FGFR3 Gene Alterations.
Tyhonas JS, Arnold LD, Cox JM, Franovic A, Gardiner E, Grandinetti K, Kania R, Kanouni T, Lardy M, Li C, Martin ES, Miller N, Mohan A, Murphy EA, Perez M, Soroceanu L, Timple N, Uryu S, Womble S, Kaldor SW. Tyhonas JS, et al. Among authors: timple n. J Med Chem. 2024 Feb 8;67(3):1734-1746. doi: 10.1021/acs.jmedchem.3c01819. Epub 2024 Jan 24. J Med Chem. 2024. PMID: 38267212
The Discovery of Exarafenib (KIN-2787): Overcoming the Challenges of Pan-RAF Kinase Inhibition.
Chen YK, Kanouni T, Arnold LD, Cox JM, Gardiner E, Grandinetti K, Jiang P, Kaldor SW, Lee C, Li C, Martin ES, Miller N, Murphy EA, Timple N, Tyhonas JS, Vassar A, Wang TS, Williams R, Yuan D, Kania RS. Chen YK, et al. Among authors: timple n. J Med Chem. 2024 Feb 8;67(3):1747-1757. doi: 10.1021/acs.jmedchem.3c01830. Epub 2024 Jan 17. J Med Chem. 2024. PMID: 38230963
EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor.
Jia Y, Juarez J, Li J, Manuia M, Niederst MJ, Tompkins C, Timple N, Vaillancourt MT, Pferdekamper AC, Lockerman EL, Li C, Anderson J, Costa C, Liao D, Murphy E, DiDonato M, Bursulaya B, Lelais G, Barretina J, McNeill M, Epple R, Marsilje TH, Pathan N, Engelman JA, Michellys PY, McNamara P, Harris J, Bender S, Kasibhatla S. Jia Y, et al. Among authors: timple n. Cancer Res. 2016 Mar 15;76(6):1591-602. doi: 10.1158/0008-5472.CAN-15-2581. Epub 2016 Jan 29. Cancer Res. 2016. PMID: 26825170
EC144 is a potent inhibitor of the heat shock protein 90.
Shi J, Van de Water R, Hong K, Lamer RB, Weichert KW, Sandoval CM, Kasibhatla SR, Boehm MF, Chao J, Lundgren K, Timple N, Lough R, Ibanez G, Boykin C, Burrows FJ, Kehry MR, Yun TJ, Harning EK, Ambrose C, Thompson J, Bixler SA, Dunah A, Snodgrass-Belt P, Arndt J, Enyedy IJ, Li P, Hong VS, McKenzie A, Biamonte MA. Shi J, et al. Among authors: timple n. J Med Chem. 2012 Sep 13;55(17):7786-95. doi: 10.1021/jm300810x. Epub 2012 Aug 31. J Med Chem. 2012. PMID: 22938030
Design, synthesis, and biological evaluation of pyrazolopyrimidine-sulfonamides as potent multiple-mitotic kinase (MMK) inhibitors (part I).
Zhang L, Fan J, Chong JH, Cesena A, Tam BY, Gilson C, Boykin C, Wang D, Aivazian D, Marcotte D, Xiao G, Le Brazidec JY, Piao J, Lundgren K, Hong K, Vu K, Nguyen K, Gan LS, Silvian L, Ling L, Teng M, Reff M, Takeda N, Timple N, Wang Q, Morena R, Khan S, Zhao S, Li T, Lee WC, Taveras AG, Chao J. Zhang L, et al. Among authors: timple n. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5633-7. doi: 10.1016/j.bmcl.2011.06.129. Epub 2011 Jul 13. Bioorg Med Chem Lett. 2011. PMID: 21798738
BIIB021, an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90.
Lundgren K, Zhang H, Brekken J, Huser N, Powell RE, Timple N, Busch DJ, Neely L, Sensintaffar JL, Yang YC, McKenzie A, Friedman J, Scannevin R, Kamal A, Hong K, Kasibhatla SR, Boehm MF, Burrows FJ. Lundgren K, et al. Among authors: timple n. Mol Cancer Ther. 2009 Apr;8(4):921-9. doi: 10.1158/1535-7163.MCT-08-0758. Mol Cancer Ther. 2009. PMID: 19372565