Optimization of a pyrazolo[1,5-a]pyrimidine class of KDR kinase inhibitors: improvements in physical properties enhance cellular activity and pharmacokinetics

Mark E. Fraley, Robert S. Rubino, William F. Hoffman, +11

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryBiochemistryKdr Kinase InhibitorsCellular ActivityMedicine +10

Kinesin spindle protein (KSP) inhibitors. Part 2: The design, synthesis, and characterization of 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP

Mark E. Fraley, R. M. Garbaccio, Kenneth L. Arrington, +20

Bioorganic & Medicinal Chemistry Letters

Protein FunctionBiochemistryNatural SciencesMolecular BiologyKinesin Spindle Protein +4

An Inhibitor of the Kinesin Spindle Protein Activates the Intrinsic Apoptotic Pathway Independently of p53 and De Novo Protein Synthesis

Weikang Tao, Victoria J. South, Ronald E. Diehl, +5

Molecular and Cellular Biology

MitophagyProtein FunctionCompetent Spindle CheckpointCell RegulationCell Division +12

Optimization of the indolyl quinolinone class of KDR (VEGFR-2) kinase inhibitors

Mark E. Fraley, Kenneth L. Arrington, Carolyn A. Buser, +12

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryPharmaceutical ScienceIndolyl Quinolinone ClassBiochemistryMedicine +10

Kinesin spindle protein (KSP) inhibitors. Part 3: Synthesis and evaluation of phenolic 2,4-diaryl-2,5-dihydropyrroles with reduced hERG binding and employment of a phosphate prodrug strategy for aqueous solubility

R. M. Garbaccio, Mark E. Fraley, Edward S. Tasber, +21

Bioorganic & Medicinal Chemistry Letters

Protein ChemistryMedicinal ChemistryPharmaceutical ScienceBiochemistryReduced Herg Binding +9

3-(Indol-2-yl)indazoles as Chek1 kinase inhibitors: Optimization of potency and selectivity via substitution at C6

Mark E. Fraley, Justin T. Steen, Edward J. Brnardic, +22

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryMedicineDrug DiscoveryRational Drug DesignPharmacological Agent +7

Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors

Edward J. Brnardic, R. M. Garbaccio, Mark E. Fraley, +22

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryBiochemistryMedicineNatural SciencesRational Drug Design +4

Convergent Synthesis of the NS5B Inhibitor GSK8175 Enabled by Transition Metal Catalysis

Kenneth L. Arrington, Gregg A. Barcan, Nicholas A. Calandra, +11

The Journal of Organic Chemistry

Pyridyl aminothiazoles as potent inhibitors of Chk1 with slow dissociation rates

Vadim Dudkin, Keith Rickert, Constantine Kreatsoulas, +13

Bioorganic & Medicinal Chemistry Letters

BiochemistryNatural SciencesMedicineRational Drug DesignMechanism Of Action +8

Discovery and evaluation of 3-(5-Thien-3-ylpyridin-3-yl)-1H-indoles as a novel class of KDR kinase inhibitors

Mark E. Fraley, Kenneth L. Arrington, Scott R. Hambaugh, +11

Bioorganic & Medicinal Chemistry Letters

Combinatorial ChemistryMedicinal ChemistryBiochemistryKdr Kinase InhibitorsNatural Sciences +5