Alex G Waterson

Summary

Affiliation: GlaxoSmithKline Research and Development
Country: USA

Publications

  1. ncbi request reprint Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors
    Alex G Waterson
    GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709 3398, USA
    Bioorg Med Chem Lett 16:2419-22. 2006
  2. doi request reprint Dual EGFR/ErbB-2 inhibitors from novel pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines
    Robert D Hubbard
    GlaxoSmithKline Research and Development, Research Triangle Park, NC 27709 3398, USA
    Bioorg Med Chem Lett 18:5738-40. 2008
  3. doi request reprint Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors
    Kirk L Stevens
    Department of Oncology Medicinal Chemistry, GlaxoSmithKline, Research Triangle Park, NC 27709, USA
    Bioorg Med Chem Lett 19:21-6. 2009
  4. doi request reprint Synthesis and evaluation of aniline headgroups for alkynyl thienopyrimidine dual EGFR/ErbB-2 kinase inhibitors
    Alex G Waterson
    GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709 3398, USA
    Bioorg Med Chem Lett 19:1332-6. 2009
  5. pmc 6-Ethynylthieno[3,2-d]- and 6-ethynylthieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB kinases
    Edgar R Wood
    Department of Assay Development, GlaxoSmithKline, Research Triangle Park, NC 27709, USA
    Proc Natl Acad Sci U S A 105:2773-8. 2008
  6. doi request reprint Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup
    John C Stellwagen
    GlaxoSmithKline Oncology CEDD, Research Triangle Park, NC 27709 3398, United States
    Bioorg Med Chem Lett 21:4436-40. 2011
  7. doi request reprint Room-temperature Pd-catalyzed amidation of aryl bromides using tert-butyl carbamate
    Swapna Bhagwanth
    Department of Medicinal Chemistry, Cancer Research, Oncology R and D, GlaxoSmithKline, Research Triangle Park, North Carolina 27709, USA
    J Org Chem 74:4634-7. 2009

Detail Information

Publications7

  1. ncbi request reprint Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors
    Alex G Waterson
    GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709 3398, USA
    Bioorg Med Chem Lett 16:2419-22. 2006
    ..In addition, the presence of a potential hydrogen bond donor appended to this ring was favored. Selected molecules in the series demonstrated some activity against human tumor cell lines...
  2. doi request reprint Dual EGFR/ErbB-2 inhibitors from novel pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines
    Robert D Hubbard
    GlaxoSmithKline Research and Development, Research Triangle Park, NC 27709 3398, USA
    Bioorg Med Chem Lett 18:5738-40. 2008
    ..Selected molecules, including compound 15h, were found to be potent in enzymatic and cellular assays while also demonstrating exposure in the mouse from an oral dose...
  3. doi request reprint Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors
    Kirk L Stevens
    Department of Oncology Medicinal Chemistry, GlaxoSmithKline, Research Triangle Park, NC 27709, USA
    Bioorg Med Chem Lett 19:21-6. 2009
    ..In addition, the impact of the absolute stereochemical configuration on cellular potency and oral mouse pharmacokinetics is described...
  4. doi request reprint Synthesis and evaluation of aniline headgroups for alkynyl thienopyrimidine dual EGFR/ErbB-2 kinase inhibitors
    Alex G Waterson
    GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709 3398, USA
    Bioorg Med Chem Lett 19:1332-6. 2009
    ..Potent inhibition of enzyme activity and cellular proliferation was observed. In certain instances, protein binding was reduced and oral exposure was found to be somewhat improved relative to compounds containing the reference aniline...
  5. pmc 6-Ethynylthieno[3,2-d]- and 6-ethynylthieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB kinases
    Edgar R Wood
    Department of Assay Development, GlaxoSmithKline, Research Triangle Park, NC 27709, USA
    Proc Natl Acad Sci U S A 105:2773-8. 2008
    ..Several ErbB family enzyme and cell potent 6-ethynyl thienopyrimidine kinase inhibitors were found to form covalent adducts with EGFR...
  6. doi request reprint Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup
    John C Stellwagen
    GlaxoSmithKline Oncology CEDD, Research Triangle Park, NC 27709 3398, United States
    Bioorg Med Chem Lett 21:4436-40. 2011
    ..The key structural features of the series are an arylsulfonamide headgroup, a thiazole core, and a fluorine ortho to the sulfonamide nitrogen...
  7. doi request reprint Room-temperature Pd-catalyzed amidation of aryl bromides using tert-butyl carbamate
    Swapna Bhagwanth
    Department of Medicinal Chemistry, Cancer Research, Oncology R and D, GlaxoSmithKline, Research Triangle Park, North Carolina 27709, USA
    J Org Chem 74:4634-7. 2009
    ..CHCl(3) and a monodentate ligand, tert-butyl X-Phos. Use of sodium tert-butoxide is crucial to the success of the reaction, which proceeds in 43-83% yield...