INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology

Eddy W. Yue, Richard Sparks, Padmaja Polam, +23

ACS Medicinal Chemistry Letters

Discovery of Potent Competitive Inhibitors of Indoleamine 2,3-Dioxygenase with in Vivo Pharmacodynamic Activity and Efficacy in a Mouse Melanoma Model

Eddy W. Yue, Brent Douty, Brian Wayland, +16

Journal of Medicinal Chemistry

PharmacotherapyVivo Pharmacodynamic ActivityPharmaceutical ChemistryTumor BiologyMedicinal Chemistry +15

Structure-Based Design and Discovery of Protein Tyrosine Phosphatase Inhibitors Incorporating Novel Isothiazolidinone Heterocyclic Phosphotyrosine Mimetics

Andrew P. Combs, Eddy W. Yue, Michael J. Bower, +30

Journal of Medicinal Chemistry

Molecular DockingCrystal StructureMedicinal ChemistryCombinatorial ChemistryBiochemistry +11

Structural Basis for Inhibition of Protein-tyrosine Phosphatase 1B by Isothiazolidinone Heterocyclic Phosphonate Mimetics

J. Paul, Lucie Gonneville, Milton C. Hillman, +14

Journal of Biological Chemistry

Structural Insights into the Design of Nonpeptidic Isothiazolidinone-containing Inhibitors of Protein-tyrosine Phosphatase 1B

J. Paul, Lucie Gonneville, Milton C. Hillman, +14

Journal of Biological Chemistry

Isothiazolidinone inhibitors of PTP1B containing imidazoles and imidazolines

Brent Douty, Brian Wayland, J. Paul, +11

Bioorganic & Medicinal Chemistry Letters

Isothiazolidinone InhibitorsMedicinal ChemistryBiochemistryMedicineNatural Sciences +6

INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ)

Eddy W. Yue, Yunlong Li, Brent Douty, +28

ACS Medicinal Chemistry Letters

Isothiazolidinone heterocycles as inhibitors of protein tyrosine phosphatases: Synthesis and structure–activity relationships of a peptide scaffold

Eddy W. Yue, Brian Wayland, Brent Douty, +13

Bioorganic & Medicinal Chemistry

BiochemistryMedicinePeptide ScaffoldIsothiazolidinone HeterocyclesPeptide Synthesis +4

Synthesis of Bridged Medium-Sized Rings through the Intramolecular Pauson−Khand Reaction

Carl J. Lovely, Hemalatha Seshadri, Brian Wayland, +1

Organic Letters

Materials ScienceExperimental SynthesisCross-coupling ReactionDerivativesEngineering +12

An intramolecular cycloaddition approach to pyrrolo[3,2- c ]quinolones

Yong He, Hossen Mahmud, Brian Wayland, +2

Tetrahedron Letters

HeterocyclicIntramolecular Cycloaddition ApproachOrganic ChemistryHeterocycle ChemistryPharmacology