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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: ruggeri ba. 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: ruggeri ba. 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
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: ruggeri ba. 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: ruggeri ba. J Med Chem. 2011 Sep 22;54(18):6328-41. doi: 10.1021/jm200758k. Epub 2011 Aug 22. J Med Chem. 2011. PMID: 21859094
Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent.
Hudkins RL, Becknell NC, Zulli AL, Underiner TL, Angeles TS, Aimone LD, Albom MS, Chang H, Miknyoczki SJ, Hunter K, Jones-Bolin S, Zhao H, Bacon ER, Mallamo JP, Ator MA, Ruggeri BA. Hudkins RL, et al. Among authors: ruggeri ba. J Med Chem. 2012 Jan 26;55(2):903-13. doi: 10.1021/jm201449n. Epub 2012 Jan 6. J Med Chem. 2012. PMID: 22148921
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: ruggeri ba. 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 a potent inhibitor of anaplastic lymphoma kinase with in vivo antitumor activity.
Ott GR, Tripathy R, Cheng M, McHugh R, Anzalone AV, Underiner TL, Curry MA, Quail MR, Lu L, Wan W, Angeles TS, Albom MS, Aimone LD, Ator MA, Ruggeri BA, Dorsey BD. Ott GR, et al. Among authors: ruggeri ba. ACS Med Chem Lett. 2010 Sep 1;1(9):493-8. doi: 10.1021/ml100158s. eCollection 2010 Dec 9. ACS Med Chem Lett. 2010. PMID: 24900237 Free PMC article.
70 results