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Fragment-Based Approach to the Development of an Orally Bioavailable Lactam Inhibitor of Lipoprotein-Associated Phospholipase A2 (Lp-PLA2).
Woolford AJ, Day PJ, Bénéton V, Berdini V, Coyle JE, Dudit Y, Grondin P, Huet P, Lee LY, Manas ES, McMenamin RL, Murray CW, Page LW, Patel VK, Potvain F, Rich SJ, Sang Y, Somers DO, Trottet L, Wan Z, Zhang X. Woolford AJ, et al. Among authors: somers do. J Med Chem. 2016 Dec 8;59(23):10738-10749. doi: 10.1021/acs.jmedchem.6b01427. Epub 2016 Nov 18. J Med Chem. 2016. PMID: 27933945
N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.
Angell RM, Atkinson FL, Brown MJ, Chuang TT, Christopher JA, Cichy-Knight M, Dunn AK, Hightower KE, Malkakorpi S, Musgrave JR, Neu M, Rowland P, Shea RL, Smith JL, Somers DO, Thomas SA, Thompson G, Wang R. Angell RM, et al. Among authors: somers do. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1296-301. doi: 10.1016/j.bmcl.2006.12.003. Epub 2006 Dec 15. Bioorg Med Chem Lett. 2007. PMID: 17194588
Biphenyl amide p38 kinase inhibitors 2: Optimisation and SAR.
Angell RM, Angell TD, Bamborough P, Brown D, Brown M, Buckton JB, Cockerill SG, Edwards CD, Jones KL, Longstaff T, Smee PA, Smith KJ, Somers DO, Walker AL, Willson M. Angell RM, et al. Among authors: somers do. Bioorg Med Chem Lett. 2008 Jan 1;18(1):324-8. doi: 10.1016/j.bmcl.2007.10.043. Epub 2007 Oct 17. Bioorg Med Chem Lett. 2008. PMID: 17981461
Biphenyl amide p38 kinase inhibitors 1: Discovery and binding mode.
Angell RM, Bamborough P, Cleasby A, Cockerill SG, Jones KL, Mooney CJ, Somers DO, Walker AL. Angell RM, et al. Among authors: somers do. Bioorg Med Chem Lett. 2008 Jan 1;18(1):318-23. doi: 10.1016/j.bmcl.2007.10.076. Epub 2007 Nov 19. Bioorg Med Chem Lett. 2008. PMID: 18006306
Pyrazolopyridines as a novel structural class of potent and selective PDE4 inhibitors.
Hamblin JN, Angell TD, Ballantine SP, Cook CM, Cooper AW, Dawson J, Delves CJ, Jones PS, Lindvall M, Lucas FS, Mitchell CJ, Neu MY, Ranshaw LE, Solanke YE, Somers DO, Wiseman JO. Hamblin JN, et al. Among authors: somers do. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4237-41. doi: 10.1016/j.bmcl.2008.05.052. Epub 2008 May 17. Bioorg Med Chem Lett. 2008. PMID: 18539455
Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.
Angell RM, Angell TD, Bamborough P, Bamford MJ, Chung CW, Cockerill SG, Flack SS, Jones KL, Laine DI, Longstaff T, Ludbrook S, Pearson R, Smith KJ, Smee PA, Somers DO, Walker AL. Angell RM, et al. Among authors: somers do. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4433-7. doi: 10.1016/j.bmcl.2008.06.028. Epub 2008 Jun 12. Bioorg Med Chem Lett. 2008. PMID: 18602262
Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity.
Angell R, Aston NM, Bamborough P, Buckton JB, Cockerill S, deBoeck SJ, Edwards CD, Holmes DS, Jones KL, Laine DI, Patel S, Smee PA, Smith KJ, Somers DO, Walker AL. Angell R, et al. Among authors: somers do. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4428-32. doi: 10.1016/j.bmcl.2008.06.048. Epub 2008 Jun 18. Bioorg Med Chem Lett. 2008. PMID: 18614366
Kinase array design, back to front: biaryl amides.
Baldwin I, Bamborough P, Haslam CG, Hunjan SS, Longstaff T, Mooney CJ, Patel S, Quinn J, Somers DO. Baldwin I, et al. Among authors: somers do. Bioorg Med Chem Lett. 2008 Oct 1;18(19):5285-9. doi: 10.1016/j.bmcl.2008.08.051. Epub 2008 Aug 22. Bioorg Med Chem Lett. 2008. PMID: 18789685
Quinolines as a novel structural class of potent and selective PDE4 inhibitors: optimisation for oral administration.
Lunniss CJ, Cooper AW, Eldred CD, Kranz M, Lindvall M, Lucas FS, Neu M, Preston AG, Ranshaw LE, Redgrave AJ, Ed Robinson J, Shipley TJ, Solanke YE, Somers DO, Wiseman JO. Lunniss CJ, et al. Among authors: somers do. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1380-5. doi: 10.1016/j.bmcl.2009.01.045. Epub 2009 Jan 19. Bioorg Med Chem Lett. 2009. PMID: 19195882
43 results