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Page 1
Identification of highly efficacious glucocorticoid receptor agonists with a potential for reduced clinical bone side effects.
Harcken C, Riether D, Kuzmich D, Liu P, Betageri R, Ralph M, Emmanuel M, Reeves JT, Berry A, Souza D, Nelson RM, Kukulka A, Fadra TN, Zuvela-Jelaska L, Dinallo R, Bentzien J, Nabozny GH, Thomson DS. Harcken C, et al. Among authors: fadra tn. J Med Chem. 2014 Feb 27;57(4):1583-98. doi: 10.1021/jm4019178. Epub 2014 Feb 7. J Med Chem. 2014. PMID: 24506830
Trifluoromethyl group as a pharmacophore: effect of replacing a CF3 group on binding and agonist activity of a glucocorticoid receptor ligand.
Betageri R, Zhang Y, Zindell RM, Kuzmich D, Kirrane TM, Bentzien J, Cardozo M, Capolino AJ, Fadra TN, Nelson RM, Paw Z, Shih DT, Shih CK, Zuvela-Jelaska L, Nabozny G, Thomson DS. Betageri R, et al. Among authors: fadra tn. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4761-9. doi: 10.1016/j.bmcl.2005.07.025. Bioorg Med Chem Lett. 2005. PMID: 16112571
Non-steroidal dissociated glucocorticoid agonists: indoles as A-ring mimetics and function-regulating pharmacophores.
Betageri R, Gilmore T, Kuzmich D, Kirrane TM, Bentzien J, Wiedenmayer D, Bekkali Y, Regan J, Berry A, Latli B, Kukulka AJ, Fadra TN, Nelson RM, Goldrick S, Zuvela-Jelaska L, Souza D, Pelletier J, Dinallo R, Panzenbeck M, Torcellini C, Lee H, Pack E, Harcken C, Nabozny G, Thomson DS. Betageri R, et al. Among authors: fadra tn. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6842-51. doi: 10.1016/j.bmcl.2011.09.018. Epub 2011 Sep 10. Bioorg Med Chem Lett. 2011. PMID: 21963986
Discovery and design of benzimidazolone based inhibitors of p38 MAP kinase.
Hammach A, Barbosa A, Gaenzler FC, Fadra T, Goldberg D, Hao MH, Kroe RR, Liu P, Qian KC, Ralph M, Sarko C, Soleymanzadeh F, Moss N. Hammach A, et al. Bioorg Med Chem Lett. 2006 Dec 15;16(24):6316-20. doi: 10.1016/j.bmcl.2006.09.014. Epub 2006 Sep 28. Bioorg Med Chem Lett. 2006. PMID: 17010605
Discovery and optimization of p38 inhibitors via computer-assisted drug design.
Goldberg DR, Hao MH, Qian KC, Swinamer AD, Gao DA, Xiong Z, Sarko C, Berry A, Lord J, Magolda RL, Fadra T, Kroe RR, Kukulka A, Madwed JB, Martin L, Pargellis C, Skow D, Song JJ, Tan Z, Torcellini CA, Zimmitti CS, Yee NK, Moss N. Goldberg DR, et al. J Med Chem. 2007 Aug 23;50(17):4016-26. doi: 10.1021/jm070415w. Epub 2007 Jul 20. J Med Chem. 2007. PMID: 17658737
Discovery and characterization of the N-phenyl-N'-naphthylurea class of p38 kinase inhibitors.
Cirillo PF, Hickey ER, Moss N, Breitfelder S, Betageri R, Fadra T, Gaenzler F, Gilmore T, Goldberg DR, Kamhi V, Kirrane T, Kroe RR, Madwed J, Moriak M, Netherton M, Pargellis CA, Patel UR, Qian KC, Sharma R, Sun S, Swinamer A, Torcellini C, Takahashi H, Tsang M, Xiong Z. Cirillo PF, et al. Bioorg Med Chem Lett. 2009 May 1;19(9):2386-91. doi: 10.1016/j.bmcl.2009.03.104. Epub 2009 Mar 26. Bioorg Med Chem Lett. 2009. PMID: 19356929