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1,236 results

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Page 1
Preclinical pharmacology of AZD5363, an inhibitor of AKT: pharmacodynamics, antitumor activity, and correlation of monotherapy activity with genetic background.
Davies BR, Greenwood H, Dudley P, Crafter C, Yu DH, Zhang J, Li J, Gao B, Ji Q, Maynard J, Ricketts SA, Cross D, Cosulich S, Chresta CC, Page K, Yates J, Lane C, Watson R, Luke R, Ogilvie D, Pass M. Davies BR, et al. Among authors: page k. Mol Cancer Ther. 2012 Apr;11(4):873-87. doi: 10.1158/1535-7163.MCT-11-0824-T. Epub 2012 Jan 31. Mol Cancer Ther. 2012. PMID: 22294718 Clinical Trial.
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. Among authors: page k. J Med Chem. 2013 Mar 14;56(5):2059-73. doi: 10.1021/jm301762v. Epub 2013 Feb 26. J Med Chem. 2013. PMID: 23394218
Discovery of 1-(4-(5-(5-amino-6-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)-1-ethyl-1,2,4-triazol-3-yl)piperidin-1-yl)-3-hydroxypropan-1-one (AZD8835): A potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment of cancers.
Barlaam B, Cosulich S, Delouvrié B, Ellston R, Fitzek M, Germain H, Green S, Hancox U, Harris CS, Hudson K, Lambert-van der Brempt C, Lebraud H, Magnien F, Lamorlette M, Le Griffon A, Morgentin R, Ouvry G, Page K, Pasquet G, Polanska U, Ruston L, Saleh T, Vautier M, Ward L. Barlaam B, et al. Among authors: page k. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5155-62. doi: 10.1016/j.bmcl.2015.10.002. Epub 2015 Oct 9. Bioorg Med Chem Lett. 2015. PMID: 26475521
Design of selective PI3Kα inhibitors starting from a promiscuous pan kinase scaffold.
Barlaam B, Cosulich S, Fitzek M, Green S, Harris CS, Hudson K, Lambert-van der Brempt C, Ouvry G, Page K, Ruston L, Ward L, Delouvrié B. Barlaam B, et al. Among authors: page k. Bioorg Med Chem Lett. 2015 Jul 1;25(13):2679-85. doi: 10.1016/j.bmcl.2015.04.084. Epub 2015 Apr 29. Bioorg Med Chem Lett. 2015. PMID: 25980912
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: page k. 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 novel aminopyrazine series as selective PI3Kα inhibitors.
Barlaam B, Cosulich S, Fitzek M, Germain H, Green S, Hanson LL, Harris CS, Hancox U, Hudson K, Lambert-van der Brempt C, Lamorlette M, Magnien F, Ouvry G, Page K, Ruston L, Ward L, Delouvrié B. Barlaam B, et al. Among authors: page k. Bioorg Med Chem Lett. 2017 Jul 1;27(13):3030-3035. doi: 10.1016/j.bmcl.2017.05.028. Epub 2017 May 10. Bioorg Med Chem Lett. 2017. PMID: 28526367
(1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): a potent and highly selective cathepsin K inhibitor for the treatment of osteoarthritis.
Dossetter AG, Beeley H, Bowyer J, Cook CR, Crawford JJ, Finlayson JE, Heron NM, Heyes C, Highton AJ, Hudson JA, Jestel A, Kenny PW, Krapp S, Martin S, MacFaul PA, McGuire TM, Gutierrez PM, Morley AD, Morris JJ, Page KM, Ribeiro LR, Sawney H, Steinbacher S, Smith C, Vickers M. Dossetter AG, et al. J Med Chem. 2012 Jul 26;55(14):6363-74. doi: 10.1021/jm3007257. Epub 2012 Jul 10. J Med Chem. 2012. PMID: 22742641
Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition.
Dossetter AG, Bowyer J, Cook CR, Crawford JJ, Finlayson JE, Heron NM, Heyes C, Highton AJ, Hudson JA, Jestel A, Krapp S, MacFaul PA, McGuire TM, Morley AD, Morris JJ, Page KM, Ribeiro LR, Sawney H, Steinbacher S, Smith C. Dossetter AG, et al. Bioorg Med Chem Lett. 2012 Sep 1;22(17):5563-8. doi: 10.1016/j.bmcl.2012.07.012. Epub 2012 Jul 15. Bioorg Med Chem Lett. 2012. PMID: 22858142
1,236 results