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Tetrahydroisoquinolines affect the whole-cell phenotype of Mycobacterium tuberculosis by inhibiting the ATP-dependent MurE ligase.
Guzman JD, Pesnot T, Barrera DA, Davies HM, McMahon E, Evangelopoulos D, Mortazavi PN, Munshi T, Maitra A, Lamming ED, Angell R, Gershater MC, Redmond JM, Needham D, Ward JM, Cuca LE, Hailes HC, Bhakta S. Guzman JD, et al. Among authors: angell r. J Antimicrob Chemother. 2015;70(6):1691-703. doi: 10.1093/jac/dkv010. Epub 2015 Feb 4. J Antimicrob Chemother. 2015. PMID: 25656411 Free PMC article.
Discovery of Sisunatovir (RV521), an Inhibitor of Respiratory Syncytial Virus Fusion.
Cockerill GS, Angell RM, Bedernjak A, Chuckowree I, Fraser I, Gascon-Simorte J, Gilman MSA, Good JAD, Harland R, Johnson SM, Ludes-Meyers JH, Littler E, Lumley J, Lunn G, Mathews N, McLellan JS, Paradowski M, Peeples ME, Scott C, Tait D, Taylor G, Thom M, Thomas E, Villalonga Barber C, Ward SE, Watterson D, Williams G, Young P, Powell K. Cockerill GS, et al. Among authors: angell rm. J Med Chem. 2021 Apr 8;64(7):3658-3676. doi: 10.1021/acs.jmedchem.0c01882. Epub 2021 Mar 17. J Med Chem. 2021. PMID: 33729773
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. 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
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: angell td. 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
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. 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. 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. 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
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. 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
84 results