Therapeutic targeting of EP300/CBP by bromodomain inhibition in hematologic malignancies

Luciano Nicosia, Gary J. Spencer, Nigel Brooks, +20

Cancer Cell

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

[3.3] Sigmatropy within 1-vinyl-2-alkenyl-7,7-dimethyl-exo-norbornan-2-ols. The first atropselective oxyanionic Cope rearrangement

Leo A. Paquette, Neil Pegg, Dana S. Toops, +2

Journal of the American Chemical Society

Cross-coupling ReactionMolecular SciencesEngineeringAlkene MetathesisChemical Analysis +9

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

Identification of 2,3-diaryl-pyrazolo[1,5-b]pyridazines as potent and selective cyclooxygenase-2 inhibitors

Paul Beswick, Sharon Bingham, C. Bountra, +21

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryBiochemistryMedicineNatural SciencesPharmacological Agent +6

Direct oxygenation of enolates generated by anionic oxy-Cope rearrangement. Expedient preparation of polycyclic .alpha.-hydroxy ketones

Leo A. Paquette, Donald T. DeRussy, Neil Pegg, +2

The Journal of Organic Chemistry

Enantioselective SynthesisEngineeringHeterocyclicBiochemistryNatural Sciences +11

Tetrazole NK1 receptor antagonists: The identification of an exceptionally potent orally active antiemetic compound

Duncan Armour, Kyeongwoon Chung, Miles Congreve, +10

Bioorganic & Medicinal Chemistry Letters

Pharmaceutical ScienceMedicineImmunologyPharmacological AgentPharmacotherapy +5

The synthesis of a conformationally restrained, combined thromboxane antagonist / synthase inhibitor using an intramolecular ‘Stille’- or ‘Grigg’-palladium-catalysed cyclisation strategy

Harry Finch, Neil Pegg, Brian Evans

Tetrahedron Letters

Medicinal ChemistryBiochemistryMedicineNatural SciencesCyclisation Strategy +6

3-substituted-1,2,4-oxadiazolin-5-one; A useful amidine precursor and protecting group

R. Bolton, Steven J. Coote, Harry Finch, +3

Tetrahedron Letters

Useful Amidine PrecursorMedicineHeterocycle ChemistryPharmacologyPharmaceutical Chemistry +1

Synthesis of grevillins, novel pyrandione pigments of fungi. Biogenetic interrelationships between grevillins, pulvinic acids, terphenylquinones and xylerythrins

Gerald Pattenden, Neil Pegg, Ronald W. Kenyon

Journal of the Chemical Society Perkin Transactions 1

Industrial MycologyNovel Pyrandione PigmentsBiosynthesisBioorganic ChemistryEngineering +12