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Page 1
New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site.
Moss N, Breitfelder S, Betageri R, Cirillo PF, Fadra T, Hickey ER, Kirrane T, Kroe RR, Madwed J, Nelson RM, Pargellis CA, Qian KC, Regan J, Swinamer A, Torcellini C. Moss N, et al. Among authors: madwed j. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4242-7. doi: 10.1016/j.bmcl.2007.05.042. Epub 2007 May 18. Bioorg Med Chem Lett. 2007. PMID: 17560108
Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796).
Regan J, Capolino A, Cirillo PF, Gilmore T, Graham AG, Hickey E, Kroe RR, Madwed J, Moriak M, Nelson R, Pargellis CA, Swinamer A, Torcellini C, Tsang M, Moss N. Regan J, et al. Among authors: madwed j. J Med Chem. 2003 Oct 23;46(22):4676-86. doi: 10.1021/jm030121k. J Med Chem. 2003. PMID: 14561087
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. Among authors: madwed j. 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
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. Among authors: madwed jb. J Med Chem. 2007 Aug 23;50(17):4016-26. doi: 10.1021/jm070415w. Epub 2007 Jul 20. J Med Chem. 2007. PMID: 17658737
Indole RSK inhibitors. Part 2: optimization of cell potency and kinase selectivity.
Kirrane TM, Boyer SJ, Burke J, Guo X, Snow RJ, Soleymanzadeh L, Swinamer A, Zhang Y, Madwed JB, Kashem M, Kugler S, O'Neill MM. Kirrane TM, et al. Among authors: madwed jb. Bioorg Med Chem Lett. 2012 Jan 1;22(1):738-42. doi: 10.1016/j.bmcl.2011.10.029. Epub 2011 Oct 18. Bioorg Med Chem Lett. 2012. PMID: 22056746
Indole RSK inhibitors. Part 1: discovery and initial SAR.
Boyer SJ, Burke J, Guo X, Kirrane TM, Snow RJ, Zhang Y, Sarko C, Soleymanzadeh L, Swinamer A, Westbrook J, Dicapua F, Padyana A, Cogan D, Gao A, Xiong Z, Madwed JB, Kashem M, Kugler S, O'Neill MM. Boyer SJ, et al. Among authors: madwed jb. Bioorg Med Chem Lett. 2012 Jan 1;22(1):733-7. doi: 10.1016/j.bmcl.2011.10.030. Epub 2011 Oct 14. Bioorg Med Chem Lett. 2012. PMID: 22100312
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: madwed jb. J Med Chem. 2012 Aug 23;55(16):7114-40. doi: 10.1021/jm300601d. Epub 2012 Aug 6. J Med Chem. 2012. PMID: 22803959
35 results