Preclinical Evaluation of AMG 900, a Novel Potent and Highly Selective Pan-Aurora Kinase Inhibitor with Activity in Taxane-Resistant Tumor Cell Lines

Marc Payton, Tammy L. Bush, Grace Chung, +18

Cancer Research

Cell DeathNovel PotentCancer BiologyGliomaTumor Biology +16

Evolution of a Highly Selective and Potent 2-(Pyridin-2-yl)-1,3,5-triazine Tie-2 Kinase Inhibitor

Brian L. Hodous, Stephanie Geuns-Meyer, Paul E. Hughes, +25

Journal of Medicinal Chemistry

Molecular BiologyPharmacotherapyChemical BiologyTumor AngiogenesisTumor Biology +19

Discovery of Aminoquinazolines as Potent, Orally Bioavailable Inhibitors of Lck:  Synthesis, SAR, and in Vivo Anti-Inflammatory Activity

Erin F. DiMauro, John Newcomb, Joseph J. Nunes, +38

Journal of Medicinal Chemistry

Pharmaceutical ScienceImmunologyImmunologic MechanismPharmacotherapyImmunotherapeutics +18

Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase

Victor J. Cee, Alan C. Cheng, Karina Romero, +22

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryPharmaceutical ScienceTie-2 KinaseBiochemistryMedicine +10

Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity

Laurie B. Schenkel, Philip R. Olivieri, Alessandro A. Boezio, +14

Journal of Medicinal Chemistry

Pain MedicineMolecular PainPharmacotherapyPain PathwaysSelective Antagonist +15

Analysis of Kinase Inhibitor Selectivity using a Thermodynamics-Based Partition Index

Alan C. Cheng, John Eksterowicz, Stephanie Geuns-Meyer, +1

Journal of Medicinal Chemistry

Drug TargetEngineeringHit IdentificationKinase Profiling PanelsThermodynamic Modelling +18

Discovery of <i>N</i>-(4-(3-(2-Aminopyrimidin-4-yl)pyridin-2-yloxy)phenyl)-4-(4-methylthiophen-2-yl)phthalazin-1-amine (AMG 900), A Highly Selective, Orally Bioavailable Inhibitor of Aurora Kinases with Activity against Multidrug-Resistant Cancer Cell Lines

Stephanie Geuns-Meyer, Victor J. Cee, Holly L. Deak, +24

Journal of Medicinal Chemistry

PharmacotherapyPharmaceutical ChemistryTumor BiologyPhysical PropertiesMolecular Pharmacology +17

Discovery of Potent and Highly Selective Thienopyridine Janus Kinase 2 Inhibitors

Laurie B. Schenkel, Xin Huang, Alan C. Cheng, +19

Journal of Medicinal Chemistry

Discovery of a Potent, Selective, and Orally Bioavailable Pyridinyl-Pyrimidine Phthalazine Aurora Kinase Inhibitor

Victor J. Cee, Laurie B. Schenkel, Brian L. Hodous, +28

Journal of Medicinal Chemistry

Pharmaceutical ScienceChemoprevention StrategyKinase InhibitorsChemical BiologyTumor Biology +14

Synthesis of 4-Substituted Chlorophthalazines, Dihydrobenzoazepinediones, 2-Pyrazolylbenzoic Acid, and 2-Pyrazolylbenzohydrazide via 3-Substituted 3-Hydroxyisoindolin-1-ones

Hanh Nho Nguyen, Victor J. Cee, Holly L. Deak, +11

The Journal of Organic Chemistry

Heterocyclic4-Substituted Chlorophthalazines2-Pyrazolylbenzoic AcidGeneral Three-step SynthesisOrganic Chemistry +7