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Page 1
Nonsteroidal glucocorticoid agonists: tetrahydronaphthalenes with alternative steroidal A-ring mimetics possessing dissociated (transrepression/transactivation) efficacy selectivity.
Biggadike K, Boudjelal M, Clackers M, Coe DM, Demaine DA, Hardy GW, Humphreys D, Inglis GG, Johnston MJ, Jones HT, House D, Loiseau R, Needham D, Skone PA, Uings I, Veitch G, Weingarten GG, McLay IM, Macdonald SJ. Biggadike K, et al. Among authors: uings i. J Med Chem. 2007 Dec 27;50(26):6519-34. doi: 10.1021/jm070778w. Epub 2007 Nov 27. J Med Chem. 2007. PMID: 18038970
Dissociated nonsteroidal glucocorticoid receptor modulators; discovery of the agonist trigger in a tetrahydronaphthalene-benzoxazine series.
Barker M, Clackers M, Copley R, Demaine DA, Humphreys D, Inglis GG, Johnston MJ, Jones HT, Haase MV, House D, Loiseau R, Nisbet L, Pacquet F, Skone PA, Shanahan SE, Tape D, Vinader VM, Washington M, Uings I, Upton R, McLay IM, Macdonald SJ. Barker M, et al. Among authors: uings i. J Med Chem. 2006 Jul 13;49(14):4216-31. doi: 10.1021/jm060302x. J Med Chem. 2006. PMID: 16821781
Non-steroidal glucocorticoid agonists: the discovery of aryl pyrazoles as A-ring mimetics.
Clackers M, Coe DM, Demaine DA, Hardy GW, Humphreys D, Inglis GG, Johnston MJ, Jones HT, House D, Loiseau R, Minick DJ, Skone PA, Uings I, McLay IM, Macdonald SJ. Clackers M, et al. Among authors: uings i. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4737-45. doi: 10.1016/j.bmcl.2007.06.066. Epub 2007 Jun 26. Bioorg Med Chem Lett. 2007. PMID: 17616395
Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists.
Biggadike K, Caivano M, Clackers M, Coe DM, Hardy GW, Humphreys D, Jones HT, House D, Miles-Williams A, Skone PA, Uings I, Weller V, McLay IM, Macdonald SJ. Biggadike K, et al. Among authors: uings i. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4846-50. doi: 10.1016/j.bmcl.2009.06.020. Epub 2009 Jun 13. Bioorg Med Chem Lett. 2009. PMID: 19592247
Design and x-ray crystal structures of high-potency nonsteroidal glucocorticoid agonists exploiting a novel binding site on the receptor.
Biggadike K, Bledsoe RK, Coe DM, Cooper TW, House D, Iannone MA, Macdonald SJ, Madauss KP, McLay IM, Shipley TJ, Taylor SJ, Tran TB, Uings IJ, Weller V, Williams SP. Biggadike K, et al. Proc Natl Acad Sci U S A. 2009 Oct 27;106(43):18114-9. doi: 10.1073/pnas.0909125106. Epub 2009 Oct 12. Proc Natl Acad Sci U S A. 2009. PMID: 19822747 Free PMC article.
Discovery of a potent series of non-steroidal non α-trifluoromethyl carbinol glucocorticoid receptor agonists with reduced lipophilicity.
Diallo H, Angell DC, Barnett HA, Biggadike K, Coe DM, Cooper TW, Craven A, Gray JR, House D, Jack TI, Keeling SP, Macdonald SJ, McLay IM, Oliver S, Taylor SJ, Uings IJ, Wellaway N. Diallo H, et al. Among authors: uings ij. Bioorg Med Chem Lett. 2011 Feb 15;21(4):1126-33. doi: 10.1016/j.bmcl.2010.12.121. Epub 2010 Dec 31. Bioorg Med Chem Lett. 2011. PMID: 21257309
Aryl aminopyrazole benzamides as oral non-steroidal selective glucocorticoid receptor agonists.
Barnett HA, Coe DM, Cooper TW, Jack TI, Jones HT, Macdonald SJ, McLay IM, Rayner N, Sasse RZ, Shipley TJ, Skone PA, Somers GI, Taylor S, Uings IJ, Woolven JM, Weingarten GG. Barnett HA, et al. Among authors: uings ij. Bioorg Med Chem Lett. 2009 Jan 1;19(1):158-62. doi: 10.1016/j.bmcl.2008.10.128. Epub 2008 Nov 5. Bioorg Med Chem Lett. 2009. PMID: 19019676
Designing corticosteroid drugs for pulmonary selectivity.
Biggadike K, Uings I, Farrow SN. Biggadike K, et al. Among authors: uings i. Proc Am Thorac Soc. 2004;1(4):352-5. doi: 10.1513/pats.200409-048TA. Proc Am Thorac Soc. 2004. PMID: 16113457 Review.
52 results