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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: skone pa. J Med Chem. 2007 Dec 27;50(26):6519-34. doi: 10.1021/jm070778w. Epub 2007 Nov 27. J Med Chem. 2007. PMID: 18038970
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: skone pa. 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
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: skone pa. 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: skone pa. 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: skone pa. 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
Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.
Liddle J, Atkinson FL, Barker MD, Carter PS, Curtis NR, Davis RP, Douault C, Dickson MC, Elwes D, Garton NS, Gray M, Hayhow TG, Hobbs CI, Jones E, Leach S, Leavens K, Lewis HD, McCleary S, Neu M, Patel VK, Preston AG, Ramirez-Molina C, Shipley TJ, Skone PA, Smithers N, Somers DO, Walker AL, Watson RJ, Weingarten GG. Liddle J, et al. Among authors: skone pa. Bioorg Med Chem Lett. 2011 Oct 15;21(20):6188-94. doi: 10.1016/j.bmcl.2011.07.082. Epub 2011 Aug 12. Bioorg Med Chem Lett. 2011. PMID: 21903390
N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of Lck: indazoles as phenol isosteres with improved pharmacokinetics.
Bamborough P, Angell RM, Bhamra I, Brown D, Bull J, Christopher JA, Cooper AW, Fazal LH, Giordano I, Hind L, Patel VK, Ranshaw LE, Sims MJ, Skone PA, Smith KJ, Vickerstaff E, Washington M. Bamborough P, et al. Among authors: skone pa. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4363-8. doi: 10.1016/j.bmcl.2007.04.029. Epub 2007 Apr 13. Bioorg Med Chem Lett. 2007. PMID: 17600705