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Page 1
Discovery of Novel UDP-N-Acetylglucosamine Acyltransferase (LpxA) Inhibitors with Activity against Pseudomonas aeruginosa.
Ryan MD, Parkes AL, Corbett D, Dickie AP, Southey M, Andersen OA, Stein DB, Barbeau OR, Sanzone A, Thommes P, Barker J, Cain R, Compper C, Dejob M, Dorali A, Etheridge D, Evans S, Faulkner A, Gadouleau E, Gorman T, Haase D, Holbrow-Wilshaw M, Krulle T, Li X, Lumley C, Mertins B, Napier S, Odedra R, Papadopoulos K, Roumpelakis V, Spear K, Trimby E, Williams J, Zahn M, Keefe AD, Zhang Y, Soutter HT, Centrella PA, Clark MA, Cuozzo JW, Dumelin CE, Deng B, Hunt A, Sigel EA, Troast DM, DeJonge BLM. Ryan MD, et al. Among authors: thommes p. J Med Chem. 2021 Oct 14;64(19):14377-14425. doi: 10.1021/acs.jmedchem.1c00888. Epub 2021 Sep 27. J Med Chem. 2021. PMID: 34569791
Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity.
Foote KM, Blades K, Cronin A, Fillery S, Guichard SS, Hassall L, Hickson I, Jacq X, Jewsbury PJ, McGuire TM, Nissink JW, Odedra R, Page K, Perkins P, Suleman A, Tam K, Thommes P, Broadhurst R, Wood C. Foote KM, et al. Among authors: thommes p. J Med Chem. 2013 Mar 14;56(5):2125-38. doi: 10.1021/jm301859s. Epub 2013 Mar 1. J Med Chem. 2013. PMID: 23394205
Discovery of a potent boronic acid derived inhibitor of the HCV RNA-dependent RNA polymerase.
Maynard A, Crosby RM, Ellis B, Hamatake R, Hong Z, Johns BA, Kahler KM, Koble C, Leivers A, Leivers MR, Mathis A, Peat AJ, Pouliot JJ, Roberts CD, Samano V, Schmidt RM, Smith GK, Spaltenstein A, Stewart EL, Thommes P, Turner EM, Voitenleitner C, Walker JT, Waitt G, Weatherhead J, Weaver K, Williams S, Wright L, Xiong ZZ, Haigh D, Shotwell JB. Maynard A, et al. Among authors: thommes p. J Med Chem. 2014 Mar 13;57(5):1902-13. doi: 10.1021/jm400317w. Epub 2013 May 29. J Med Chem. 2014. PMID: 23672667
1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity.
Cano C, Saravanan K, Bailey C, Bardos J, Curtin NJ, Frigerio M, Golding BT, Hardcastle IR, Hummersone MG, Menear KA, Newell DR, Richardson CJ, Shea K, Smith GC, Thommes P, Ting A, Griffin RJ. Cano C, et al. Among authors: thommes p. J Med Chem. 2013 Aug 22;56(16):6386-401. doi: 10.1021/jm400915j. Epub 2013 Aug 1. J Med Chem. 2013. PMID: 23855836
Optimization of novel acyl pyrrolidine inhibitors of hepatitis C virus RNA-dependent RNA polymerase leading to a development candidate.
Slater MJ, Amphlett EM, Andrews DM, Bravi G, Burton G, Cheasty AG, Corfield JA, Ellis MR, Fenwick RH, Fernandes S, Guidetti R, Haigh D, Hartley CD, Howes PD, Jackson DL, Jarvest RL, Lovegrove VL, Medhurst KJ, Parry NR, Price H, Shah P, Singh OM, Stocker R, Thommes P, Wilkinson C, Wonacott A. Slater MJ, et al. Among authors: thommes p. J Med Chem. 2007 Mar 8;50(5):897-900. doi: 10.1021/jm061207r. Epub 2007 Feb 2. J Med Chem. 2007. PMID: 17269759
Synthesis and evaluation of novel alpha-amino cyclic boronates as inhibitors of HCV NS3 protease.
Li X, Zhang YK, Liu Y, Ding CZ, Li Q, Zhou Y, Plattner JJ, Baker SJ, Qian X, Fan D, Liao L, Ni ZJ, White GV, Mordaunt JE, Lazarides LX, Slater MJ, Jarvest RL, Thommes P, Ellis M, Edge CM, Hubbard JA, Somers D, Rowland P, Nassau P, McDowell B, Skarzynski TJ, Kazmierski WM, Grimes RM, Wright LL, Smith GK, Zou W, Wright J, Pennicott LE. Li X, et al. Among authors: thommes p. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3550-6. doi: 10.1016/j.bmcl.2010.04.129. Epub 2010 May 20. Bioorg Med Chem Lett. 2010. PMID: 20493689
Novel macrocyclic HCV NS3 protease inhibitors derived from α-amino cyclic boronates.
Li X, Zhang YK, Liu Y, Ding CZ, Zhou Y, Li Q, Plattner JJ, Baker SJ, Zhang S, Kazmierski WM, Wright LL, Smith GK, Grimes RM, Crosby RM, Creech KL, Carballo LH, Slater MJ, Jarvest RL, Thommes P, Hubbard JA, Convery MA, Nassau PM, McDowell W, Skarzynski TJ, Qian X, Fan D, Liao L, Ni ZJ, Pennicott LE, Zou W, Wright J. Li X, et al. Among authors: thommes p. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5695-700. doi: 10.1016/j.bmcl.2010.08.022. Epub 2010 Aug 10. Bioorg Med Chem Lett. 2010. PMID: 20801653
46 results