Chunze Li

Summary

Affiliation: Pfizer Global Research and Development
Country: USA

Publications

  1. doi Stereospecific reduction of a potent kinesin spindle protein (KSP) inhibitor in human tissues
    Chunze Li
    Department of Drug Metabolism and Pharmacokinetics, West Point, PA 19486, USA
    Biochem Pharmacol 79:1526-33. 2010
  2. ncbi Kinesin spindle protein (KSP) inhibitors. Part 7: Design and synthesis of 3,3-disubstituted dihydropyrazolobenzoxazines as potent inhibitors of the mitotic kinesin KSP
    Robert M Garbaccio
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:5671-6. 2007
  3. doi Kinesin spindle protein (KSP) inhibitors. 9. Discovery of (2S)-4-(2,5-difluorophenyl)-n-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the treatment of taxane-refractory can
    Christopher D Cox
    Department of Medicinal Chemistry, Merck Research Laboratories, P O Box 4, Sumneytown Pike, West Point, Pennsylvania 19486, USA
    J Med Chem 51:4239-52. 2008
  4. ncbi Kinesin spindle protein (KSP) inhibitors. Part 6: Design and synthesis of 3,5-diaryl-4,5-dihydropyrazole amides as potent inhibitors of the mitotic kinesin KSP
    Paul J Coleman
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, Sumneytown Pike, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:5390-5. 2007
  5. ncbi Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP
    Anthony J Roecker
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, Sumneytown Pike, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:5677-82. 2007
  6. ncbi Rifampin induces the in vitro oxidative metabolism, but not the in vivo clearance of diclofenac in rhesus monkeys
    Thomayant Prueksaritanont
    Department of Drug Metabolism, WP 75 100, Merck Research Laboratories, West Point, PA 19486, USA
    Drug Metab Dispos 34:1806-10. 2006
  7. ncbi Discovery of a potent, CNS-penetrant orexin receptor antagonist based on an n,n-disubstituted-1,4-diazepane scaffold that promotes sleep in rats
    David B Whitman
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, WP14 2, West Point, PA 19486, USA
    ChemMedChem 4:1069-74. 2009
  8. ncbi In vitro and in vivo CYP3A64 induction and inhibition studies in rhesus monkeys: a preclinical approach for CYP3A-mediated drug interaction studies
    Thomayant Prueksaritanont
    Department of Drug Metabolism, WP75 100, Merck Research Laboratories, West Point, PA 19486, USA
    Drug Metab Dispos 34:1546-55. 2006
  9. doi Proline bis-amides as potent dual orexin receptor antagonists
    Jeffrey M Bergman
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 18:1425-30. 2008
  10. ncbi Acyl-coenzyme a formation of simvastatin in mouse liver preparations
    Chunze Li
    Department of Drug Metabolism, Merck Research Laboratories, West Point, PA 19486, USA
    Drug Metab Dispos 34:102-10. 2006

Collaborators

Detail Information

Publications12

  1. doi Stereospecific reduction of a potent kinesin spindle protein (KSP) inhibitor in human tissues
    Chunze Li
    Department of Drug Metabolism and Pharmacokinetics, West Point, PA 19486, USA
    Biochem Pharmacol 79:1526-33. 2010
    ..Collectively, the results implicated the aldo-keto reductase 1Cs as the most likely enzymes responsible for the metabolic interconversion of Compound A and its active metabolite M1...
  2. ncbi Kinesin spindle protein (KSP) inhibitors. Part 7: Design and synthesis of 3,3-disubstituted dihydropyrazolobenzoxazines as potent inhibitors of the mitotic kinesin KSP
    Robert M Garbaccio
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:5671-6. 2007
    ..The synthesis is highlighted by a key [3+2] cycloaddition to form the pyrazolobenzoxazine core followed by diastereospecific installation of a quaternary center...
  3. doi Kinesin spindle protein (KSP) inhibitors. 9. Discovery of (2S)-4-(2,5-difluorophenyl)-n-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the treatment of taxane-refractory can
    Christopher D Cox
    Department of Medicinal Chemistry, Merck Research Laboratories, P O Box 4, Sumneytown Pike, West Point, Pennsylvania 19486, USA
    J Med Chem 51:4239-52. 2008
    ..Compound 30 (MK-0731) was recently studied in a phase I clinical trial in patients with taxane-refractory solid tumors...
  4. ncbi Kinesin spindle protein (KSP) inhibitors. Part 6: Design and synthesis of 3,5-diaryl-4,5-dihydropyrazole amides as potent inhibitors of the mitotic kinesin KSP
    Paul J Coleman
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, Sumneytown Pike, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:5390-5. 2007
    ..Careful adjustment of amine basicity was essential for preserving cellular potency in a multidrug resistant cell line while maintaining good aqueous solubility...
  5. ncbi Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP
    Anthony J Roecker
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, Sumneytown Pike, West Point, PA 19486, USA
    Bioorg Med Chem Lett 17:5677-82. 2007
    ..Crystallographic evidence of binding mode and in vivo potency data is also highlighted...
  6. ncbi Rifampin induces the in vitro oxidative metabolism, but not the in vivo clearance of diclofenac in rhesus monkeys
    Thomayant Prueksaritanont
    Department of Drug Metabolism, WP 75 100, Merck Research Laboratories, West Point, PA 19486, USA
    Drug Metab Dispos 34:1806-10. 2006
    ....
  7. ncbi Discovery of a potent, CNS-penetrant orexin receptor antagonist based on an n,n-disubstituted-1,4-diazepane scaffold that promotes sleep in rats
    David B Whitman
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, WP14 2, West Point, PA 19486, USA
    ChemMedChem 4:1069-74. 2009
    ..In telemetry-implanted rats, oral administration of this antagonist produced a decrease in wakefulness, while increasing REM and non-REM sleep...
  8. ncbi In vitro and in vivo CYP3A64 induction and inhibition studies in rhesus monkeys: a preclinical approach for CYP3A-mediated drug interaction studies
    Thomayant Prueksaritanont
    Department of Drug Metabolism, WP75 100, Merck Research Laboratories, West Point, PA 19486, USA
    Drug Metab Dispos 34:1546-55. 2006
    ..These findings suggest the potential applicability of the in vitro-in vivo relationship approach in rhesus monkeys for studying CYP3A-mediated interactions in humans...
  9. doi Proline bis-amides as potent dual orexin receptor antagonists
    Jeffrey M Bergman
    Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
    Bioorg Med Chem Lett 18:1425-30. 2008
    ..A compound from this series has demonstrated in vivo central activity when dosed peripherally in a pharmacodynamic model of orexin activity...
  10. ncbi Acyl-coenzyme a formation of simvastatin in mouse liver preparations
    Chunze Li
    Department of Drug Metabolism, Merck Research Laboratories, West Point, PA 19486, USA
    Drug Metab Dispos 34:102-10. 2006
    ....
  11. ncbi Kinesin spindle protein (KSP) inhibitors. Part 4: Structure-based design of 5-alkylamino-3,5-diaryl-4,5-dihydropyrazoles as potent, water-soluble inhibitors of the mitotic kinesin KSP
    Christopher D Cox
    Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, Sumneytown Pike, West Point, PA 19486, USA
    Bioorg Med Chem Lett 16:3175-9. 2006
    ..This change led to a second generation compound with increased potency, a 400-fold enhancement in aqueous solubility at pH 4, and improved dog pharmacokinetics relative to the first generation compound...
  12. ncbi Comparative effects of fibrates on drug metabolizing enzymes in human hepatocytes
    Thomayant Prueksaritanont
    Department of Drug Metabolism, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
    Pharm Res 22:71-8. 2005
    ..The induction potential of different fibric acid derivatives on human drug metabolizing enzymes was evaluated to help assess the role of enzyme induction on pharmacokinetic drug interactions...