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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: bentzien j. 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: bentzien j. 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
Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists.
Regan J, Lee TW, Zindell RM, Bekkali Y, Bentzien J, Gilmore T, Hammach A, Kirrane TM, Kukulka AJ, Kuzmich D, Nelson RM, Proudfoot JR, Ralph M, Pelletier J, Souza D, Zuvela-Jelaska L, Nabozny G, Thomson DS. Regan J, et al. Among authors: bentzien j. J Med Chem. 2006 Dec 28;49(26):7887-96. doi: 10.1021/jm061273t. J Med Chem. 2006. PMID: 17181172
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: bentzien j. 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 of a potent and dissociated non-steroidal glucocorticoid receptor agonist containing an alkyl carbinol pharmacophore.
Razavi H, Riether D, Harcken C, Bentzien J, Dinallo RM, Souza D, Nelson RM, Kukulka A, Fadra-Khan TN, Pack EJ Jr, Zuvela-Jelaska L, Pelletier J, Panzenbeck M, Torcellini CA, Proudfoot JR, Nabozny GH, Thomson DS. Razavi H, et al. Among authors: bentzien j. Bioorg Med Chem Lett. 2014 Apr 15;24(8):1934-40. doi: 10.1016/j.bmcl.2014.03.005. Epub 2014 Mar 12. Bioorg Med Chem Lett. 2014. PMID: 24656565
5-Aminomethylbenzimidazoles as potent ITK antagonists.
Riether D, Zindell R, Kowalski JA, Cook BN, Bentzien J, Lombaert SD, Thomson D, Kugler SZ Jr, Skow D, Martin LS, Raymond EL, Khine HH, O'Shea K, Woska JR Jr, Jeanfavre D, Sellati R, Ralph KL, Ahlberg J, Labissiere G, Kashem MA, Pullen SS, Takahashi H. Riether D, et al. Among authors: bentzien j. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1588-91. doi: 10.1016/j.bmcl.2009.02.012. Epub 2009 Feb 8. Bioorg Med Chem Lett. 2009. PMID: 19246196
Identification of a potent sodium hydrogen exchanger isoform 1 (NHE1) inhibitor with a suitable profile for chronic dosing and demonstrated cardioprotective effects in a preclinical model of myocardial infarction in the rat.
Huber JD, Bentzien J, Boyer SJ, Burke J, De Lombaert S, Eickmeier C, Guo X, Haist JV, Hickey ER, Kaplita P, Karmazyn M, Kemper R, Kennedy CA, Kirrane T, Madwed JB, Mainolfi E, Nagaraja N, Soleymanzadeh F, Swinamer A, Eldrup AB. Huber JD, et al. Among authors: bentzien j. J Med Chem. 2012 Aug 23;55(16):7114-40. doi: 10.1021/jm300601d. Epub 2012 Aug 6. J Med Chem. 2012. PMID: 22803959
24 results