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Page 1
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: hudson 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
Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors.
Hennequin LF, Ballard P, Boyle FT, Delouvrié B, Ellston RP, Halsall CT, Harris CS, Hudson K, Kendrew J, Pease JE, Ross HS, Smith P, Vincent JL. Hennequin LF, et al. Among authors: hudson k. Bioorg Med Chem Lett. 2006 May 15;16(10):2672-6. doi: 10.1016/j.bmcl.2006.02.025. Epub 2006 Mar 3. Bioorg Med Chem Lett. 2006. PMID: 16516473
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: hudson 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
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: hudson 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
A new series of neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.
Barlaam B, Ballard P, Bradbury RH, Ducray R, Germain H, Hickinson DM, Hudson K, Kettle JG, Klinowska T, Magnien F, Ogilvie DJ, Olivier A, Pearson SE, Scott JS, Suleman A, Trigwell CB, Vautier M, Whittaker RD, Wood R. Barlaam B, et al. Among authors: hudson k. Bioorg Med Chem Lett. 2008 Jan 15;18(2):674-8. doi: 10.1016/j.bmcl.2007.11.052. Epub 2007 Nov 21. Bioorg Med Chem Lett. 2008. PMID: 18061446
Neutral 5-substituted 4-indazolylaminoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.
Barlaam B, Acton DG, Ballard P, Bradbury RH, Cross D, Ducray R, Germain H, Hudson K, Klinowska T, Magnien F, Ogilvie DJ, Olivier A, Ross HS, Smith R, Trigwell CB, Vautier M, Wright L. Barlaam B, et al. Among authors: hudson k. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1799-803. doi: 10.1016/j.bmcl.2008.02.035. Epub 2008 Feb 16. Bioorg Med Chem Lett. 2008. PMID: 18313293
Intermittent High-Dose Scheduling of AZD8835, a Novel Selective Inhibitor of PI3Kα and PI3Kδ, Demonstrates Treatment Strategies for PIK3CA-Dependent Breast Cancers.
Hudson K, Hancox UJ, Trigwell C, McEwen R, Polanska UM, Nikolaou M, Morentin Gutierrez P, Avivar-Valderas A, Delpuech O, Dudley P, Hanson L, Ellston R, Jones A, Cumberbatch M, Cosulich SC, Ward L, Cruzalegui F, Green S. Hudson K, et al. Mol Cancer Ther. 2016 May;15(5):877-89. doi: 10.1158/1535-7163.MCT-15-0687. Epub 2016 Feb 2. Mol Cancer Ther. 2016. PMID: 26839307
Design and synthesis of novel lactate dehydrogenase A inhibitors by fragment-based lead generation.
Ward RA, Brassington C, Breeze AL, Caputo A, Critchlow S, Davies G, Goodwin L, Hassall G, Greenwood R, Holdgate GA, Mrosek M, Norman RA, Pearson S, Tart J, Tucker JA, Vogtherr M, Whittaker D, Wingfield J, Winter J, Hudson K. Ward RA, et al. Among authors: hudson k. J Med Chem. 2012 Apr 12;55(7):3285-306. doi: 10.1021/jm201734r. Epub 2012 Mar 26. J Med Chem. 2012. PMID: 22417091
520 results