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Discovery and optimization of a series of 3-(3-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: orally bioavailable, selective, and potent ATP-independent Akt inhibitors.
Ashwell MA, Lapierre JM, Brassard C, Bresciano K, Bull C, Cornell-Kennon S, Eathiraj S, France DS, Hall T, Hill J, Kelleher E, Khanapurkar S, Kizer D, Koerner S, Link J, Liu Y, Makhija S, Moussa M, Namdev N, Nguyen K, Nicewonger R, Palma R, Szwaya J, Tandon M, Uppalapati U, Vensel D, Volak LP, Volckova E, Westlund N, Wu H, Yang RY, Chan TC. Ashwell MA, et al. Among authors: kizer d. J Med Chem. 2012 Jun 14;55(11):5291-310. doi: 10.1021/jm300276x. Epub 2012 May 31. J Med Chem. 2012. PMID: 22533986
Discovery of 3-(3-(4-(1-Aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine (ARQ 092): An Orally Bioavailable, Selective, and Potent Allosteric AKT Inhibitor.
Lapierre JM, Eathiraj S, Vensel D, Liu Y, Bull CO, Cornell-Kennon S, Iimura S, Kelleher EW, Kizer DE, Koerner S, Makhija S, Matsuda A, Moussa M, Namdev N, Savage RE, Szwaya J, Volckova E, Westlund N, Wu H, Schwartz B. Lapierre JM, et al. Among authors: kizer de. J Med Chem. 2016 Jul 14;59(13):6455-69. doi: 10.1021/acs.jmedchem.6b00619. Epub 2016 Jun 29. J Med Chem. 2016. PMID: 27305487
Piperidine-based heterocyclic oxalyl amides as potent p38 alpha MAP kinase inhibitors.
Mavunkel BJ, Perumattam JJ, Tan X, Luedtke GR, Lu Q, Lim D, Kizer D, Dugar S, Chakravarty S, Xu YJ, Jung J, Liclican A, Levy DE, Tabora J. Mavunkel BJ, et al. Among authors: kizer d. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1059-62. doi: 10.1016/j.bmcl.2009.12.031. Epub 2009 Dec 11. Bioorg Med Chem Lett. 2010. PMID: 20031411
Inhibiting TGF-beta signaling restores immune surveillance in the SMA-560 glioma model.
Tran TT, Uhl M, Ma JY, Janssen L, Sriram V, Aulwurm S, Kerr I, Lam A, Webb HK, Kapoun AM, Kizer DE, McEnroe G, Hart B, Axon J, Murphy A, Chakravarty S, Dugar S, Protter AA, Higgins LS, Wick W, Weller M, Wong DH. Tran TT, et al. Among authors: kizer de. Neuro Oncol. 2007 Jul;9(3):259-70. doi: 10.1215/15228517-2007-010. Epub 2007 May 23. Neuro Oncol. 2007. PMID: 17522330 Free PMC article.
66 results