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Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.
Rowbottom MW, Faraoni R, Chao Q, Campbell BT, Lai AG, Setti E, Ezawa M, Sprankle KG, Abraham S, Tran L, Struss B, Gibney M, Armstrong RC, Gunawardane RN, Nepomuceno RR, Valenta I, Hua H, Gardner MF, Cramer MD, Gitnick D, Insko DE, Apuy JL, Jones-Bolin S, Ghose AK, Herbertz T, Ator MA, Dorsey BD, Ruggeri B, Williams M, Bhagwat S, James J, Holladay MW. Rowbottom MW, et al. Among authors: hua h. J Med Chem. 2012 Feb 9;55(3):1082-105. doi: 10.1021/jm2009925. Epub 2012 Jan 23. J Med Chem. 2012. PMID: 22168626
Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors.
Abraham S, Hadd MJ, Tran L, Vickers T, Sindac J, Milanov ZV, Holladay MW, Bhagwat SS, Hua H, Ford Pulido JM, Cramer MD, Gitnick D, James J, Dao A, Belli B, Armstrong RC, Treiber DK, Liu G. Abraham S, et al. Among authors: hua h. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5296-300. doi: 10.1016/j.bmcl.2011.07.027. Epub 2011 Jul 14. Bioorg Med Chem Lett. 2011. PMID: 21802948
Discovery of highly potent and selective pan-Aurora kinase inhibitors with enhanced in vivo antitumor therapeutic index.
Liu G, Abraham S, Tran L, Vickers TD, Xu S, Hadd MJ, Quiambao S, Holladay MW, Hua H, Ford Pulido JM, Gunawardane RN, Davis MI, Eichelberger SR, Apuy JL, Gitnick D, Gardner MF, James J, Breider MA, Belli B, Armstrong RC, Treiber DK. Liu G, et al. Among authors: hua h. J Med Chem. 2012 Apr 12;55(7):3250-60. doi: 10.1021/jm201702g. Epub 2012 Mar 14. J Med Chem. 2012. PMID: 22380736
1,551 results