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Page 1
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: kugler s. 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
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: kugler s. 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
Dihydrobenzisoxazole-4-one compounds are novel selective inhibitors of aldosterone synthase (CYP11B2) with in vivo activity.
Meyers K, Cogan DA, Burke J, Arenas R, Balestra M, Brown NF, Chen Z, Cerny MA, Clifford HE, Colombo F, Fader L, Frederick KS, Guo X, Goldberg D, Hornberger KR, Kugler S, Lord J, Marshall DR, Moss N, Parmentier JH, Richman JR, Schmenk J, Weldon SM, Yu M, Zhang M. Meyers K, et al. Among authors: kugler s. Bioorg Med Chem Lett. 2018 Mar 1;28(5):979-984. doi: 10.1016/j.bmcl.2017.12.015. Epub 2017 Dec 8. Bioorg Med Chem Lett. 2018. PMID: 29254646
Discovery of potent inhibitors of interleukin-2 inducible T-cell kinase (ITK) through structure-based drug design.
Cook BN, Bentzien J, White A, Nemoto PA, Wang J, Man CC, Soleymanzadeh F, Khine HH, Kashem MA, Kugler SZ Jr, Wolak JP, Roth GP, De Lombaert S, Pullen SS, Takahashi H. Cook BN, et al. Among authors: kugler sz jr. Bioorg Med Chem Lett. 2009 Feb 1;19(3):773-7. doi: 10.1016/j.bmcl.2008.12.028. Epub 2008 Dec 10. Bioorg Med Chem Lett. 2009. PMID: 19111460
Mitigation of off-target adrenergic binding and effects on cardiovascular function in the discovery of novel ribosomal S6 kinase 2 inhibitors.
Fryer RM, Muthukumarana A, Chen RR, Smith JD, Mazurek SN, Harrington KE, Dinallo RM, Burke J, DiCapua FM, Guo X, Kirrane TM, Snow RJ, Zhang Y, Soleymanzadeh F, Madwed JB, Kashem MA, Kugler SZ, O'Neill MM, Harrison PC, Reinhart GA, Boyer SJ. Fryer RM, et al. J Pharmacol Exp Ther. 2012 Mar;340(3):492-500. doi: 10.1124/jpet.111.189365. Epub 2011 Nov 29. J Pharmacol Exp Ther. 2012. PMID: 22128344
Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: part 2, optimization for blood pressure reduction in spontaneously hypertensive rats.
Ginn JD, Bosanac T, Chen R, Cywin C, Hickey E, Kashem M, Kerr S, Kugler S, Li X, Prokopowicz A 3rd, Schlyer S, Smith JD, Turner MR, Wu F, Young ER. Ginn JD, et al. Among authors: kugler s. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5153-6. doi: 10.1016/j.bmcl.2010.07.014. Epub 2010 Aug 1. Bioorg Med Chem Lett. 2010. PMID: 20678931
277 results