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Inhibitors of epidermal growth factor receptor tyrosine kinase: Novel C-5 substituted anilinoquinazolines designed to target the ribose pocket.
Ballard P, Bradbury RH, Harris CS, Hennequin LF, Hickinson M, Johnson PD, Kettle JG, Klinowska T, Leach AG, Morgentin R, Pass M, Ogilvie DJ, Olivier A, Warin N, Williams EJ. Ballard P, et al. Among authors: leach ag. Bioorg Med Chem Lett. 2006 Mar 15;16(6):1633-7. doi: 10.1016/j.bmcl.2005.12.028. Epub 2005 Dec 27. Bioorg Med Chem Lett. 2006. PMID: 16380259
Discovery of 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an orally bioavailable, potent inhibitor of Akt kinases.
Addie M, Ballard P, Buttar D, Crafter C, Currie G, Davies BR, Debreczeni J, Dry H, Dudley P, Greenwood R, Johnson PD, Kettle JG, Lane C, Lamont G, Leach A, Luke RW, Morris J, Ogilvie D, Page K, Pass M, Pearson S, Ruston L. Addie M, et al. J Med Chem. 2013 Mar 14;56(5):2059-73. doi: 10.1021/jm301762v. Epub 2013 Feb 26. J Med Chem. 2013. PMID: 23394218
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
McCoull W, Addie MS, Birch AM, Birtles S, Buckett LK, Butlin RJ, Bowker SS, Boyd S, Chapman S, Davies RD, Donald CS, Green CP, Jenner C, Kemmitt PD, Leach AG, Moody GC, Gutierrez PM, Newcombe NJ, Nowak T, Packer MJ, Plowright AT, Revill J, Schofield P, Sheldon C, Stokes S, Turnbull AV, Wang SJ, Whalley DP, Wood JM. McCoull W, et al. Among authors: leach ag. Bioorg Med Chem Lett. 2012 Jun 15;22(12):3873-8. doi: 10.1016/j.bmcl.2012.04.117. Epub 2012 May 2. Bioorg Med Chem Lett. 2012. PMID: 22608962
Discovery, optimisation and in vivo evaluation of novel GPR119 agonists.
Brocklehurst KJ, Broo A, Butlin RJ, Brown HS, Clarke DS, Davidsson Ö, Goldberg K, Groombridge SD, Kelly EE, Leach A, McKerrecher D, O'Donnell C, Poucher S, Schofield P, Scott JS, Teague J, Westgate L, Wood MJ. Brocklehurst KJ, et al. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7310-6. doi: 10.1016/j.bmcl.2011.10.033. Epub 2011 Oct 18. Bioorg Med Chem Lett. 2011. PMID: 22061639
Matched molecular pairs as a medicinal chemistry tool.
Griffen E, Leach AG, Robb GR, Warner DJ. Griffen E, et al. Among authors: leach ag. J Med Chem. 2011 Nov 24;54(22):7739-50. doi: 10.1021/jm200452d. Epub 2011 Sep 22. J Med Chem. 2011. PMID: 21936582 No abstract available.
94 results