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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: aimone ld. 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 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. Among authors: aimone ld. J Med Chem. 2003 Dec 4;46(25):5375-88. doi: 10.1021/jm0301641. J Med Chem. 2003. PMID: 14640546
Design and synthesis of dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole oximes as potent dual inhibitors of TIE-2 and VEGF-R2 receptor tyrosine kinases.
Dandu R, Zulli AL, Bacon ER, Underiner T, Robinson C, Chang H, Miknyoczki S, Grobelny J, Ruggeri BA, Yang S, Albom MS, Angeles TS, Aimone LD, Hudkins RL. Dandu R, et al. Among authors: aimone ld. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1916-21. doi: 10.1016/j.bmcl.2008.02.001. Epub 2008 Feb 7. Bioorg Med Chem Lett. 2008. PMID: 18308565
Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models.
Hudkins RL, Diebold JL, Tao M, Josef KA, Park CH, Angeles TS, Aimone LD, Husten J, Ator MA, Meyer SL, Holskin BP, Durkin JT, Fedorov AA, Fedorov EV, Almo SC, Mathiasen JR, Bozyczko-Coyne D, Saporito MS, Scott RW, Mallamo JP. Hudkins RL, et al. Among authors: aimone ld. J Med Chem. 2008 Sep 25;51(18):5680-9. doi: 10.1021/jm8005838. Epub 2008 Aug 21. J Med Chem. 2008. PMID: 18714982
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: aimone ld. 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
2,4-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: aimone ld. 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-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: aimone ld. J Med Chem. 2011 Sep 22;54(18):6328-41. doi: 10.1021/jm200758k. Epub 2011 Aug 22. J Med Chem. 2011. PMID: 21859094
67 results