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Page 1
Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
Gingrich DE, Lisko JG, Curry MA, Cheng M, Quail M, Lu L, Wan W, Albom MS, Angeles TS, Aimone LD, Haltiwanger RC, Wells-Knecht K, Ott GR, Ghose AK, Ator MA, Ruggeri B, Dorsey BD. Gingrich DE, et al. Among authors: ghose ak. J Med Chem. 2012 May 24;55(10):4580-93. doi: 10.1021/jm201550q. Epub 2012 May 7. J Med Chem. 2012. PMID: 22564207
Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase.
Milkiewicz KL, Weinberg LR, Albom MS, Angeles TS, Cheng M, Ghose AK, Roemmele RC, Theroff JP, Underiner TL, Zificsak CA, Dorsey BD. Milkiewicz KL, et al. Among authors: ghose ak. Bioorg Med Chem. 2010 Jun 15;18(12):4351-62. doi: 10.1016/j.bmc.2010.04.087. Epub 2010 Apr 29. Bioorg Med Chem. 2010. PMID: 20483621
2,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazines: new variant of an old template and application to the discovery of anaplastic lymphoma kinase (ALK) inhibitors with in vivo antitumor activity.
Ott GR, Wells GJ, Thieu TV, Quail MR, Lisko JG, Mesaros EF, Gingrich DE, Ghose AK, Wan W, Lu L, Cheng M, Albom MS, Angeles TS, Huang Z, Aimone LD, Ator MA, Ruggeri BA, Dorsey BD. Ott GR, et al. Among authors: ghose ak. J Med Chem. 2011 Sep 22;54(18):6328-41. doi: 10.1021/jm200758k. Epub 2011 Aug 22. J Med Chem. 2011. PMID: 21859094
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: ghose ak. J Med Chem. 2012 Feb 9;55(3):1082-105. doi: 10.1021/jm2009925. Epub 2012 Jan 23. J Med Chem. 2012. PMID: 22168626
Design, synthesis, and anaplastic lymphoma kinase (ALK) inhibitory activity for a novel series of 2,4,8,22-tetraazatetracyclo[14.3.1.1³,⁷.1⁹,¹³]docosa-1(20),3(22),4,6,9(21),10,12,16,18-nonaene macrocycles.
Breslin HJ, Lane BM, Ott GR, Ghose AK, Angeles TS, Albom MS, Cheng M, Wan W, Haltiwanger RC, Wells-Knecht KJ, Dorsey BD. Breslin HJ, et al. Among authors: ghose ak. J Med Chem. 2012 Jan 12;55(1):449-64. doi: 10.1021/jm201333e. Epub 2011 Dec 15. J Med Chem. 2012. PMID: 22172029
Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).
Ott GR, Cheng M, Learn KS, Wagner J, Gingrich DE, Lisko JG, Curry M, Mesaros EF, Ghose AK, Quail MR, Wan W, Lu L, Dobrzanski P, Albom MS, Angeles TS, Wells-Knecht K, Huang Z, Aimone LD, Bruckheimer E, Anderson N, Friedman J, Fernandez SV, Ator MA, Ruggeri BA, Dorsey BD. Ott GR, et al. Among authors: ghose ak. J Med Chem. 2016 Aug 25;59(16):7478-96. doi: 10.1021/acs.jmedchem.6b00487. Epub 2016 Aug 15. J Med Chem. 2016. PMID: 27527804
50 results