A Convergent Synthetic Route to (+)-Dynemicin A and Analogs of Wide Structural Variability

Andrew G. Myers, Norma J. Tom, Mark E. Fraley, +2

Journal of the American Chemical Society

Bioorganic ChemistryEngineeringIsobenzofuran 107Molecular BiologyConvergent Synthetic Route +21

Kinesin Spindle Protein (KSP) Inhibitors. 9. Discovery of (2<i>S</i>)-4-(2,5-Difluorophenyl)-<i>N</i>-[(3<i>R</i>,4<i>S</i>)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-<i>N</i>-methyl-2-phenyl-2,5-dihydro-1<i>H</i>-pyrrole-1-carboxamide (MK-0731) for the Treatment of Taxane-Refractory Cancer

Christopher D. Cox, Paul J. Coleman, Michael J. Breslin, +24

Journal of Medicinal Chemistry

Synthesis and Initial SAR Studies of 3,6-Disubstituted Pyrazolo[1,5-a]pyrimidines: A New Class of KDR Kinase Inhibitors

Mark E. Fraley, William F. Hoffman, Robert S. Rubino, +8

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryBiochemistryKdr Kinase InhibitorsInitial Sar StudiesMedicine +8

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

Synthesis of (+)-dynemicin A and analogs of wide structural variability: establishment of the absolute configuration of natural dynemicin A

Andrew G. Myers, Mark E. Fraley, Norma J. Tom, +2

Chemistry & Biology

Absolute ConfigurationBiochemistryNatural Dynemicin ANatural SciencesMolecular Biology +3

Development of thioquinazolinones, allosteric Chk1 kinase inhibitors

Antonella Converso, Timothy J. Hartingh, R. M. Garbaccio, +22

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryBiochemistryMedicineNatural SciencesPharmacotherapy +4

Characterization of Ubrogepant: A Potent and Selective Antagonist of the Human Calcitonin Gene‒Related Peptide Receptor

Eric L. Moore, Mark E. Fraley, Ian M. Bell, +9

Journal of Pharmacology and Experimental Therapeutics

Discovery of 5′′‐Chloro‐<i>N</i>‐[(5,6‐dimethoxypyridin‐2‐yl)methyl]‐2,2′:5′,3′′‐terpyridine‐3′‐carboxamide (MK‐1064): A Selective Orexin 2 Receptor Antagonist (2‐SORA) for the Treatment of Insomnia

Anthony J. Roecker, Swati P. Mercer, John D. Schreier, +20

ChemMedChem

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