Mark J Thompson

Summary

Affiliation: University of Sheffield
Country: UK

Publications

  1. doi request reprint Synthesis and evaluation of 1-amino-6-halo-β-carbolines as antimalarial and antiprion agents
    Mark J Thompson
    Department of Chemistry, University of Sheffield, Brook Hill, Sheffield, S7 3HF, UK
    ChemMedChem 7:578-86. 2012
  2. doi request reprint Improved 2,4-diarylthiazole-based antiprion agents: switching the sense of the amide group at C5 leads to an increase in potency
    Mark J Thompson
    Department of Chemistry, University of Sheffield, Brook Hill, Sheffield, S7 3HF, UK
    ChemMedChem 5:1476-88. 2010
  3. doi request reprint 2,4-diarylthiazole antiprion compounds as a novel structural class of antimalarial leads
    Mark J Thompson
    Department of Chemistry, University of Sheffield, Brook Hill, Sheffield, UK
    Bioorg Med Chem Lett 21:3644-7. 2011
  4. doi request reprint Discovery of 6-substituted indole-3-glyoxylamides as lead antiprion agents with enhanced cell line activity, improved microsomal stability and low toxicity
    Mark J Thompson
    Department of Chemistry, University of Sheffield, Krebs Institute, Brook Hill, Sheffield S3 7HF, UK
    Eur J Med Chem 46:4125-32. 2011
  5. doi request reprint Structure-activity relationship refinement and further assessment of indole-3-glyoxylamides as a lead series against prion disease
    Mark J Thompson
    Department of Chemistry, University of Sheffield, Brook Hill, UK
    ChemMedChem 6:115-30. 2011
  6. ncbi request reprint Synthesis and evaluation of a focused library of pyridine dicarbonitriles against prion disease
    Kai Guo
    Department of Chemistry, University of Sheffield, Dainton Building, Brook Hill, Sheffield S3 7HF, UK
    Eur J Med Chem 43:93-106. 2008
  7. doi request reprint Design, synthesis, and structure-activity relationship of indole-3-glyoxylamide libraries possessing highly potent activity in a cell line model of prion disease
    Mark J Thompson
    Department of Chemistry, University of Sheffield, Brook Hill, Sheffield S3 7HF, UK
    J Med Chem 52:7503-11. 2009
  8. doi request reprint Development of a diversity-oriented approach to oxazole-5-amide libraries
    Mark J Thompson
    Department of Chemistry, University of Sheffield, Brook Hill, Sheffield S3 7HF, UK
    J Org Chem 74:3856-65. 2009
  9. doi request reprint Ugi reactions with ammonia offer rapid access to a wide range of 5-aminothiazole and oxazole derivatives
    Mark J Thompson
    Department of Chemistry, University of Sheffield, Brook Hill, Sheffield S3 7HF, UK
    J Org Chem 74:7084-93. 2009
  10. doi request reprint Exploring catalyst and solvent effects in the multicomponent synthesis of pyridine-3,5-dicarbonitriles
    Kai Guo
    Department of Chemistry, University of Sheffield, Brook Hill, Sheffield S3 7HF, UK
    J Org Chem 74:6999-7006. 2009

Collaborators

Detail Information

Publications12

  1. doi request reprint Synthesis and evaluation of 1-amino-6-halo-β-carbolines as antimalarial and antiprion agents
    Mark J Thompson
    Department of Chemistry, University of Sheffield, Brook Hill, Sheffield, S7 3HF, UK
    ChemMedChem 7:578-86. 2012
    ....
  2. doi request reprint Improved 2,4-diarylthiazole-based antiprion agents: switching the sense of the amide group at C5 leads to an increase in potency
    Mark J Thompson
    Department of Chemistry, University of Sheffield, Brook Hill, Sheffield, S7 3HF, UK
    ChemMedChem 5:1476-88. 2010
    ..Evaluation of binding to cellular prion protein (PrP(C)) showed only weak affinities at best, suggesting that the newly identified antiprion agents do not mediate their biological effect through direct interaction with PrP(C)...
  3. doi request reprint 2,4-diarylthiazole antiprion compounds as a novel structural class of antimalarial leads
    Mark J Thompson
    Department of Chemistry, University of Sheffield, Brook Hill, Sheffield, UK
    Bioorg Med Chem Lett 21:3644-7. 2011
    ..In addition, three new members of the series showed superior antiprion activity compared to the earlier-reported compounds...
  4. doi request reprint Discovery of 6-substituted indole-3-glyoxylamides as lead antiprion agents with enhanced cell line activity, improved microsomal stability and low toxicity
    Mark J Thompson
    Department of Chemistry, University of Sheffield, Krebs Institute, Brook Hill, Sheffield S3 7HF, UK
    Eur J Med Chem 46:4125-32. 2011
    ..The foregoing observations thus make the indole-3-glyoxylamides an attractive lead series for continuing development as potential therapeutic agents against prion disease...
  5. doi request reprint Structure-activity relationship refinement and further assessment of indole-3-glyoxylamides as a lead series against prion disease
    Mark J Thompson
    Department of Chemistry, University of Sheffield, Brook Hill, UK
    ChemMedChem 6:115-30. 2011
    ..The present results thereby confirm the indole-3-glyoxylamides as a promising lead series for continuing in vitro and in vivo evaluation against prion disease...
  6. ncbi request reprint Synthesis and evaluation of a focused library of pyridine dicarbonitriles against prion disease
    Kai Guo
    Department of Chemistry, University of Sheffield, Dainton Building, Brook Hill, Sheffield S3 7HF, UK
    Eur J Med Chem 43:93-106. 2008
    ..5-9microwo compounds were found to reduce PrPSc levels to below 30% relative to an untreated control at 50nM...
  7. doi request reprint Design, synthesis, and structure-activity relationship of indole-3-glyoxylamide libraries possessing highly potent activity in a cell line model of prion disease
    Mark J Thompson
    Department of Chemistry, University of Sheffield, Brook Hill, Sheffield S3 7HF, UK
    J Med Chem 52:7503-11. 2009
    ..Thus, the indole-3-glyoxylamides described herein constitute ideal candidates to progress to further development as potential therapeutics for the family of human prion disorders...
  8. doi request reprint Development of a diversity-oriented approach to oxazole-5-amide libraries
    Mark J Thompson
    Department of Chemistry, University of Sheffield, Brook Hill, Sheffield S3 7HF, UK
    J Org Chem 74:3856-65. 2009
    ....
  9. doi request reprint Ugi reactions with ammonia offer rapid access to a wide range of 5-aminothiazole and oxazole derivatives
    Mark J Thompson
    Department of Chemistry, University of Sheffield, Brook Hill, Sheffield S3 7HF, UK
    J Org Chem 74:7084-93. 2009
    ..Free or N-substituted 5-aminothiazoles and 5-(trifluoroacetamido)oxazoles were all prepared by this improved methodology. The scope of the synthetic route developed and application of the different products are discussed...
  10. doi request reprint Exploring catalyst and solvent effects in the multicomponent synthesis of pyridine-3,5-dicarbonitriles
    Kai Guo
    Department of Chemistry, University of Sheffield, Brook Hill, Sheffield S3 7HF, UK
    J Org Chem 74:6999-7006. 2009
    ..A reaction intermediate, Knoevenagel adduct 7, plays the major role in the amine base-catalyzed system, while in the presence of an ionic base, aerobic oxygen acts as the primary oxidant...
  11. ncbi request reprint A small molecule modulator of prion protein increases human mesenchymal stem cell lifespan, ex vivo expansion, and engraftment to bone marrow in NOD/SCID mice
    Sindhu T Mohanty
    Mellanby Centre for Bone Research, Department of Human Metabolism, University of Sheffield, Sheffield, United Kingdom
    Stem Cells 30:1134-43. 2012
    ..These data point to PrP as a good target for chemical intervention in stem cell regenerative medicine...
  12. ncbi request reprint Library synthesis and screening: 2,4-diphenylthiazoles and 2,4-diphenyloxazoles as potential novel prion disease therapeutics
    William Heal
    Department of Chemistry, University of Sheffield, Brook Hill, Sheffield, S3 7HF, UK
    J Med Chem 50:1347-53. 2007
    ..Of the compounds prepared, 15 were found to bind to human PrPC and six showed inhibition of PrPSc formation, displaying EC50s between 1.5 and 20 microM...