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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: wells knecht kj. 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 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. J Med Chem. 2012 May 24;55(10):4580-93. doi: 10.1021/jm201550q. Epub 2012 May 7. J Med Chem. 2012. PMID: 22564207
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. 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
2,4-Diaminopyrimidine inhibitors of c-Met kinase bearing benzoxazepine anilines.
Zificsak CA, Theroff JP, Aimone LD, Albom MS, Angeles TS, Brown RA, Galinis D, Grobelny JV, Herbertz T, Husten J, Kocsis LS, LoSardo C, Miknyoczki SJ, Murthy S, Rolon-Steele D, Underiner TL, Wells-Knecht KJ, Worrell CS, Zeigler KS, Dorsey BD. Zificsak CA, et al. Among authors: wells knecht kj. Bioorg Med Chem Lett. 2011 Jan 15;21(2):660-3. doi: 10.1016/j.bmcl.2010.12.013. Epub 2010 Dec 8. Bioorg Med Chem Lett. 2011. PMID: 21190849
2,7-Pyrrolo[2,1-f][1,2,4]triazines as JAK2 inhibitors: modification of target structure to minimize reactive metabolite formation.
Weinberg LR, Albom MS, Angeles TS, Breslin HJ, Gingrich DE, Huang Z, Lisko JG, Mason JL, Milkiewicz KL, Thieu TV, Underiner TL, Wells GJ, Wells-Knecht KJ, Dorsey BD. Weinberg LR, et al. Among authors: wells knecht kj. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7325-30. doi: 10.1016/j.bmcl.2011.10.032. Epub 2011 Oct 14. Bioorg Med Chem Lett. 2011. PMID: 22041060
Strategies to mitigate the bioactivation of 2-anilino-7-aryl-pyrrolo[2,1-f][1,2,4]triazines: identification of orally bioavailable, efficacious ALK inhibitors.
Mesaros EF, Thieu TV, Wells GJ, Zificsak CA, Wagner JC, Breslin HJ, Tripathy R, Diebold JL, McHugh RJ, Wohler AT, Quail MR, Wan W, Lu L, Huang Z, Albom MS, Angeles TS, Wells-Knecht KJ, Aimone LD, Cheng M, Ator MA, Ott GR, Dorsey BD. Mesaros EF, et al. Among authors: wells knecht kj. J Med Chem. 2012 Jan 12;55(1):115-25. doi: 10.1021/jm2010767. Epub 2011 Dec 29. J Med Chem. 2012. PMID: 22141319
A selective, orally bioavailable 1,2,4-triazolo[1,5-a]pyridine-based inhibitor of Janus kinase 2 for use in anticancer therapy: discovery of CEP-33779.
Dugan BJ, Gingrich DE, Mesaros EF, Milkiewicz KL, Curry MA, Zulli AL, Dobrzanski P, Serdikoff C, Jan M, Angeles TS, Albom MS, Mason JL, Aimone LD, Meyer SL, Huang Z, Wells-Knecht KJ, Ator MA, Ruggeri BA, Dorsey BD. Dugan BJ, et al. Among authors: wells knecht kj. J Med Chem. 2012 Jun 14;55(11):5243-54. doi: 10.1021/jm300248q. Epub 2012 May 18. J Med Chem. 2012. PMID: 22594690
31 results