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Page 1
The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase.
Malagu K, Duggan H, Menear K, Hummersone M, Gomez S, Bailey C, Edwards P, Drzewiecki J, Leroux F, Quesada MJ, Hermann G, Maine S, Molyneaux CA, Le Gall A, Pullen J, Hickson I, Smith L, Maguire S, Martin N, Smith G, Pass M. Malagu K, et al. Bioorg Med Chem Lett. 2009 Oct 15;19(20):5950-3. doi: 10.1016/j.bmcl.2009.08.038. Epub 2009 Aug 13. Bioorg Med Chem Lett. 2009. PMID: 19762236
AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mammalian target of rapamycin kinase inhibitor with in vitro and in vivo antitumor activity.
Chresta CM, Davies BR, Hickson I, Harding T, Cosulich S, Critchlow SE, Vincent JP, Ellston R, Jones D, Sini P, James D, Howard Z, Dudley P, Hughes G, Smith L, Maguire S, Hummersone M, Malagu K, Menear K, Jenkins R, Jacobsen M, Smith GC, Guichard S, Pass M. Chresta CM, et al. Cancer Res. 2010 Jan 1;70(1):288-98. doi: 10.1158/0008-5472.CAN-09-1751. Epub 2009 Dec 22. Cancer Res. 2010. PMID: 20028854
Identification and optimisation of novel and selective small molecular weight kinase inhibitors of mTOR.
Menear KA, Gomez S, Malagu K, Bailey C, Blackburn K, Cockcroft XL, Ewen S, Fundo A, Le Gall A, Hermann G, Sebastian L, Sunose M, Presnot T, Torode E, Hickson I, Martin NM, Smith GC, Pike KG. Menear KA, et al. Bioorg Med Chem Lett. 2009 Oct 15;19(20):5898-901. doi: 10.1016/j.bmcl.2009.08.069. Epub 2009 Aug 21. Bioorg Med Chem Lett. 2009. PMID: 19733066
Pyranone, thiopyranone, and pyridone inhibitors of phosphatidylinositol 3-kinase related kinases. Structure-activity relationships for DNA-dependent protein kinase inhibition, and identification of the first potent and selective inhibitor of the ataxia telangiectasia mutated kinase.
Hollick JJ, Rigoreau LJ, Cano-Soumillac C, Cockcroft X, Curtin NJ, Frigerio M, Golding BT, Guiard S, Hardcastle IR, Hickson I, Hummersone MG, Menear KA, Martin NM, Matthews I, Newell DR, Ord R, Richardson CJ, Smith GC, Griffin RJ. Hollick JJ, et al. Among authors: menear ka. J Med Chem. 2007 Apr 19;50(8):1958-72. doi: 10.1021/jm061121y. Epub 2007 Mar 20. J Med Chem. 2007. PMID: 17371003
Novel alkoxybenzamide inhibitors of poly(ADP-ribose) polymerase.
Menear KA, Adcock C, Alonso FC, Blackburn K, Copsey L, Drzewiecki J, Fundo A, Le Gall A, Gomez S, Javaid H, Lence CF, Martin NM, Mydlowski C, Smith GC. Menear KA, et al. Bioorg Med Chem Lett. 2008 Jul 15;18(14):3942-5. doi: 10.1016/j.bmcl.2008.06.025. Epub 2008 Jun 12. Bioorg Med Chem Lett. 2008. PMID: 18579376
DNA-dependent protein kinase (DNA-PK) inhibitors. Synthesis and biological activity of quinolin-4-one and pyridopyrimidin-4-one surrogates for the chromen-4-one chemotype.
Cano C, Barbeau OR, Bailey C, Cockcroft XL, Curtin NJ, Duggan H, Frigerio M, Golding BT, Hardcastle IR, Hummersone MG, Knights C, Menear KA, Newell DR, Richardson CJ, Smith GC, Spittle B, Griffin RJ. Cano C, et al. Among authors: menear ka. J Med Chem. 2010 Dec 23;53(24):8498-507. doi: 10.1021/jm100608j. Epub 2010 Nov 16. J Med Chem. 2010. PMID: 21080722
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: menear ka. J Med Chem. 2013 Aug 22;56(16):6386-401. doi: 10.1021/jm400915j. Epub 2013 Aug 1. J Med Chem. 2013. PMID: 23855836
Phthalazinones. Part 1: The design and synthesis of a novel series of potent inhibitors of poly(ADP-ribose)polymerase.
Loh VM Jr, Cockcroft XL, Dillon KJ, Dixon L, Drzewiecki J, Eversley PJ, Gomez S, Hoare J, Kerrigan F, Matthews IT, Menear KA, Martin NM, Newton RF, Paul J, Smith GC, Vile J, Whittle AJ. Loh VM Jr, et al. Among authors: menear ka. Bioorg Med Chem Lett. 2005 May 2;15(9):2235-8. doi: 10.1016/j.bmcl.2005.03.026. Bioorg Med Chem Lett. 2005. PMID: 15837300
27 results