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CEP-28122, a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers.
Cheng M, Quail MR, Gingrich DE, Ott GR, Lu L, Wan W, Albom MS, Angeles TS, Aimone LD, Cristofani F, Machiorlatti R, Abele C, Ator MA, Dorsey BD, Inghirami G, Ruggeri BA. Cheng M, et al. Among authors: dorsey bd. Mol Cancer Ther. 2012 Mar;11(3):670-9. doi: 10.1158/1535-7163.MCT-11-0776. Epub 2011 Dec 27. Mol Cancer Ther. 2012. PMID: 22203728
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: dorsey bd. 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
Novel 2,3,4,5-tetrahydro-benzo[d]azepine derivatives of 2,4-diaminopyrimidine, selective and orally bioavailable ALK inhibitors with antitumor efficacy in ALCL mouse models.
Mesaros EF, Burke JP, Parrish JD, Dugan BJ, Anzalone AV, Angeles TS, Albom MS, Aimone LD, Quail MR, Wan W, Lu L, Huang Z, Ator MA, Ruggeri BA, Cheng M, Ott GR, Dorsey BD. Mesaros EF, et al. Among authors: dorsey bd. Bioorg Med Chem Lett. 2011 Jan 1;21(1):463-6. doi: 10.1016/j.bmcl.2010.10.115. Epub 2010 Oct 27. Bioorg Med Chem Lett. 2011. PMID: 21074994
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: dorsey bd. J Med Chem. 2011 Sep 22;54(18):6328-41. doi: 10.1021/jm200758k. Epub 2011 Aug 22. J Med Chem. 2011. PMID: 21859094
Depletion of autoreactive plasma cells and treatment of lupus nephritis in mice using CEP-33779, a novel, orally active, selective inhibitor of JAK2.
Lu LD, Stump KL, Wallace NH, Dobrzanski P, Serdikoff C, Gingrich DE, Dugan BJ, Angeles TS, Albom MS, Mason JL, Ator MA, Dorsey BD, Ruggeri BA, Seavey MM. Lu LD, et al. Among authors: dorsey bd. J Immunol. 2011 Oct 1;187(7):3840-53. doi: 10.4049/jimmunol.1101228. Epub 2011 Aug 31. J Immunol. 2011. PMID: 21880982
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: dorsey bd. J Med Chem. 2012 Jan 12;55(1):115-25. doi: 10.1021/jm2010767. Epub 2011 Dec 29. J Med Chem. 2012. PMID: 22141319
Optimization of a novel kinase inhibitor scaffold for the dual inhibition of JAK2 and FAK kinases.
Zificsak CA, Gingrich DE, Breslin HJ, Dunn DD, Milkiewicz KL, Theroff JP, Thieu TV, Underiner TL, Weinberg LR, Aimone LD, Albom MS, Mason JL, Saville L, Husten J, Angeles TS, Finn JP, Jan M, O'Kane TM, Dobrzanski P, Dorsey BD. Zificsak CA, et al. Among authors: dorsey bd. Bioorg Med Chem Lett. 2012 Jan 1;22(1):133-7. doi: 10.1016/j.bmcl.2011.11.049. Epub 2011 Nov 25. Bioorg Med Chem Lett. 2012. PMID: 22169263
64 results