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188 results

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Page 1
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).
Ward RA, Anderton MJ, Ashton S, Bethel PA, Box M, Butterworth S, Colclough N, Chorley CG, Chuaqui C, Cross DA, Dakin LA, Debreczeni JÉ, Eberlein C, Finlay MR, Hill GB, Grist M, Klinowska TC, Lane C, Martin S, Orme JP, Smith P, Wang F, Waring MJ. Ward RA, et al. Among authors: hill gb. J Med Chem. 2013 Sep 12;56(17):7025-48. doi: 10.1021/jm400822z. Epub 2013 Aug 30. J Med Chem. 2013. PMID: 23930994
Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.
Finlay MR, Anderton M, Ashton S, Ballard P, Bethel PA, Box MR, Bradbury RH, Brown SJ, Butterworth S, Campbell A, Chorley C, Colclough N, Cross DA, Currie GS, Grist M, Hassall L, Hill GB, James D, James M, Kemmitt P, Klinowska T, Lamont G, Lamont SG, Martin N, McFarland HL, Mellor MJ, Orme JP, Perkins D, Perkins P, Richmond G, Smith P, Ward RA, Waring MJ, Whittaker D, Wells S, Wrigley GL. Finlay MR, et al. Among authors: hill gb. J Med Chem. 2014 Oct 23;57(20):8249-67. doi: 10.1021/jm500973a. Epub 2014 Oct 1. J Med Chem. 2014. PMID: 25271963
SAR and inhibitor complex structure determination of a novel class of potent and specific Aurora kinase inhibitors.
Heron NM, Anderson M, Blowers DP, Breed J, Eden JM, Green S, Hill GB, Johnson T, Jung FH, McMiken HH, Mortlock AA, Pannifer AD, Pauptit RA, Pink J, Roberts NJ, Rowsell S. Heron NM, et al. Among authors: hill gb. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1320-3. doi: 10.1016/j.bmcl.2005.11.053. Epub 2005 Dec 5. Bioorg Med Chem Lett. 2006. PMID: 16337122
Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.
Mortlock AA, Foote KM, Heron NM, Jung FH, Pasquet G, Lohmann JJ, Warin N, Renaud F, De Savi C, Roberts NJ, Johnson T, Dousson CB, Hill GB, Perkins D, Hatter G, Wilkinson RW, Wedge SR, Heaton SP, Odedra R, Keen NJ, Crafter C, Brown E, Thompson K, Brightwell S, Khatri L, Brady MC, Kearney S, McKillop D, Rhead S, Parry T, Green S. Mortlock AA, et al. Among authors: hill gb. J Med Chem. 2007 May 3;50(9):2213-24. doi: 10.1021/jm061335f. Epub 2007 Mar 21. J Med Chem. 2007. PMID: 17373783
Synthesis and SAR of 1-acetanilide-4-aminopyrazole-substituted quinazolines: selective inhibitors of Aurora B kinase with potent anti-tumor activity.
Foote KM, Mortlock AA, Heron NM, Jung FH, Hill GB, Pasquet G, Brady MC, Green S, Heaton SP, Kearney S, Keen NJ, Odedra R, Wedge SR, Wilkinson RW. Foote KM, et al. Among authors: hill gb. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1904-9. doi: 10.1016/j.bmcl.2008.02.002. Epub 2008 Feb 7. Bioorg Med Chem Lett. 2008. PMID: 18294849
Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.
Jung FH, Pasquet G, Lambert-van der Brempt C, Lohmann JJ, Warin N, Renaud F, Germain H, De Savi C, Roberts N, Johnson T, Dousson C, Hill GB, Mortlock AA, Heron N, Wilkinson RW, Wedge SR, Heaton SP, Odedra R, Keen NJ, Green S, Brown E, Thompson K, Brightwell S. Jung FH, et al. Among authors: hill gb. J Med Chem. 2006 Feb 9;49(3):955-70. doi: 10.1021/jm050786h. J Med Chem. 2006. PMID: 16451062
Approaches to the design of anti-fibrotic drugs.
Franklin TJ, Hales NJ, Johnstone D, Morris WB, Cunliffe CJ, Millest AJ, Hill GB. Franklin TJ, et al. Among authors: hill gb. Biochem Soc Trans. 1991 Nov;19(4):812-5. doi: 10.1042/bst0190812. Biochem Soc Trans. 1991. PMID: 1665444 No abstract available.
188 results