Discovery of Novel PI3-Kinase δ Specific Inhibitors for the Treatment of Rheumatoid Arthritis: Taming CYP3A4 Time-Dependent Inhibition

Brian S. Safina, Stewart Baker, Matt Baumgardner, +44

Journal of Medicinal Chemistry

Drug TargetImmunologyInflammatory ArthritisSystems PharmacologyMolecular Pharmacology +23

Potent and selective inhibitors of PI3Kδ: Obtaining isoform selectivity from the affinity pocket and tryptophan shelf

Daniel P. Sutherlin, Stewart Baker, Angelina Bisconte, +32

Bioorganic & Medicinal Chemistry Letters

BiochemistryFunctional SelectivityMedicinePharmacologyRational Drug Design +6

1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoid receptor antagonists with high functional activity

Robin D. Clark, Nicholas C. Ray, Karen Williams, +13

Bioorganic & Medicinal Chemistry Letters

Selective Glucocorticoid ReceptorBiochemistryFunctional SelectivityMedicinePharmacological Agent +4

Solid-phase synthesis of diverse tetrahydro-1,4-benzodiazepine-2-ones

Gurdip Bhalay, Paul Blaney, Vanessa H. Palmer, +1

Tetrahedron Letters

Solid-phase SynthesisOrganic ChemistrySynthesis MethodChemistrySynthetic Chemistry

Fused and bridged bi- and tri-cyclic lactams via sequential metallo-azomethine ylide cycloaddition–lactamisation

Paul Blaney, Ronald Grigg, Zoran Ranković, +2

Tetrahedron

Cross-coupling ReactionEngineeringOrganic ChemistryChemistryTri-cyclic Lactams +2

Discovery of a First-in-Class Potent Small Molecule Antagonist against the Adrenomedullin-2 Receptor

Paris Avgoustou, Ameera B. A. Jailani, Jean‐Olivier Zirimwabagabo, +15

ACS Pharmacology & Translational Science

Solid-phase synthesis of tertiary methylamines via reductive alkylation–fragmentation using a hydroxylamine linker

Paul Blaney, Ronald Grigg, Zoran Ranković, +1

Tetrahedron Letters

Solid-phase SynthesisEngineeringOrganic ChemistryChemistrySynthesis Method +5

Application of Grignard reagents to the synthesis of tertiary methylamines via resin-bound oxyiminium ions

Paul Blaney, Ronald Grigg, Zoran Ranković, +1

Tetrahedron Letters

Chemical EngineeringEngineeringGrignard ReagentsResin-bound Oxyiminium IonsOrganic Chemistry +5

A practical synthesis of the enantiomers of hydroxychloroquine

Paul Blaney, Stephen J. Byard, Glynis Carr, +5

Tetrahedron Asymmetry

Practical SynthesisOrganic ChemistryStereoselective SynthesisChemistryPharmacology +1

2-Benzenesulfonyl-8a-benzyl-hexahydro-2H-isoquinolin-6-ones as selective glucocorticoid receptor antagonists

Robin D. Clark, Nicholas C. Ray, Paul Blaney, +10

Bioorganic & Medicinal Chemistry Letters

BiochemistryMedicinePharmacological AgentPharmacotherapyGlucocorticoid +2