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16 results

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Page 1
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: gingrich de. 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
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: gingrich de. 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: gingrich de. J Immunol. 2011 Oct 1;187(7):3840-53. doi: 10.4049/jimmunol.1101228. Epub 2011 Aug 31. J Immunol. 2011. PMID: 21880982
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: gingrich de. 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
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: gingrich de. 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
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
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: gingrich de. J Med Chem. 2012 Jun 14;55(11):5243-54. doi: 10.1021/jm300248q. Epub 2012 May 18. J Med Chem. 2012. PMID: 22594690
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: gingrich de. 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
A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the identification of CEP-5214 and its dimethylglycine ester prodrug clinical candidate CEP-7055.
Gingrich DE, Reddy DR, Iqbal MA, Singh J, Aimone LD, Angeles TS, Albom M, Yang S, Ator MA, Meyer SL, Robinson C, Ruggeri BA, Dionne CA, Vaught JL, Mallamo JP, Hudkins RL. Gingrich DE, et al. J Med Chem. 2003 Dec 4;46(25):5375-88. doi: 10.1021/jm0301641. J Med Chem. 2003. PMID: 14640546
16 results