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Identification of a Chemical Probe for Bromo and Extra C‑Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit

Journal of medicinal chemistry, 2012-11, Vol.55 (22), p.9831-9837

2012

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Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance

Science advances, 2015-11, Vol.1 (10), p.e1500723

2015

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Therapeutics for COVID-19

Nature microbiology, 2023-05, Vol.8 (5), p.771-786

2023

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Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases

Journal of medicinal chemistry, 2020-11, Vol.63 (22), p.13561-13577

2020

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One-Pot Synthesis of N-Arylpyrazoles from Arylhalides

Organic letters, 2009-05, Vol.11 (10), p.2097-2100

2009

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(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells

Proceedings of the National Academy of Sciences - PNAS, 2014-09, Vol.111 (35), p.12853-12858

2014

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Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit

Journal of medicinal chemistry, 2016-05, Vol.59 (10), p.4800-4811

2016

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Structural basis for CCR6 modulation by allosteric antagonists

Nature communications, 2024-08, Vol.15 (1), p.7574-13, Article 7574

2024

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Covalent Inhibitors of Interleukin‑2 Inducible T Cell Kinase (Itk) with Nanomolar Potency in a Whole-Blood Assay

Journal of medicinal chemistry, 2012-11, Vol.55 (22), p.10047-10063

2012

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Demonstration of In Vitro to In Vivo Translation of a TYK2 Inhibitor That Shows Cross Species Potency Differences

Scientific reports, 2020-06, Vol.10 (1), p.8974-8974, Article 8974

2020

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Design and optimization of a series of 4-(3-azabicyclo[3.1.0]hexan-3-yl)pyrimidin-2-amines: Dual inhibitors of TYK2 and JAK1

Bioorganic & medicinal chemistry, 2020-05, Vol.28 (10), p.115481-115481, Article 115481

2020

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Synthesis of Chiral Azabicycles from Pyroglutaminols

Organic letters, 2016-11, Vol.18 (21), p.5748-5751

2016

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Siderophore Receptor-Mediated Uptake of Lactivicin Analogues in Gram-Negative Bacteria

Journal of medicinal chemistry, 2014-05, Vol.57 (9), p.3845-3855

2014

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Selective Targeting of Bromodomains of the Bromodomain-PHD Fingers Family Impairs Osteoclast Differentiation

ACS chemical biology, 2017-10, Vol.12 (10), p.2619-2630

2017

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A direct copper-catalyzed route to pyrrolo-fused heterocycles from boronic acids

Tetrahedron letters, 2012-02, Vol.53 (5), p.564-569

2012

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Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841)

Journal of medicinal chemistry, 2018-10, Vol.61 (19), p.8597-8612

2018

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Pyridone-Conjugated Monobactam Antibiotics with Gram-Negative Activity

Journal of medicinal chemistry, 2013-07, Vol.56 (13), p.5541-5552

2013

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Diazonamide Support Studies: Stereoselective Formation of the C10 Chiral Center in both the CDEFG and AEFG Fragments

Organic letters, 2008-09, Vol.10 (18), p.3969-3972

2008

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Novel monobactams utilizing a siderophore uptake mechanism for the treatment of gram-negative infections

Bioorganic & medicinal chemistry letters, 2012-09, Vol.22 (18), p.5989-5994

2012

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Structural Characterization of an Enantiomerically Pure Amino Acid Imidazolide and Direct Formation of the β-Lactam Nucleus from an α-Amino Acid

Organic letters, 2008-02, Vol.10 (3), p.369-372

2008

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Carbanion Stabilization by Distal Silyloxy Groups. Origin of the High Diastereoselectivity in the Formation of Quaternary Centers with Aryllead(IV) Triacetate Reagents

Organic letters, 2002-11, Vol.4 (23), p.4121-4124

2002

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One-pot copper-catalyzed synthesis of N-functionalized pyrazoles from boronic acids

Tetrahedron letters, 2010, Vol.51 (38), p.5005-5008

2010

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ChemInform Abstract: A Direct Copper-Catalyzed Route to Pyrrolo-Fused Heterocycles from Boronic Acids

ChemInform, 2012-05, Vol.43 (20), p.no-no

2012

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Corrigendum to “Novel monobactams utilizing a siderophore uptake mechanism for the treatment of Gram-negative infections” [Bioorg. Med. Chem. Lett. 22/18 (2012) 5989–5994]

Bioorganic & medicinal chemistry letters, 2015-09, Vol.25 (18), p.4029-4029

2015

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tert-Buyldiphenylsilylethyl (“TBDPSE”): A Practical Protecting Group for Phenols

Journal of organic chemistry, 2005-02, Vol.70 (4), p.1467-1470

2005

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Identification of a Chemical Probe for Bromo and Extra C‑Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit

Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance

Therapeutics for COVID-19

Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases

One-Pot Synthesis of N-Arylpyrazoles from Arylhalides

(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells

Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit

Structural basis for CCR6 modulation by allosteric antagonists

Covalent Inhibitors of Interleukin‑2 Inducible T Cell Kinase (Itk) with Nanomolar Potency in a Whole-Blood Assay

Demonstration of In Vitro to In Vivo Translation of a TYK2 Inhibitor That Shows Cross Species Potency Differences

Design and optimization of a series of 4-(3-azabicyclo[3.1.0]hexan-3-yl)pyrimidin-2-amines: Dual inhibitors of TYK2 and JAK1

Synthesis of Chiral Azabicycles from Pyroglutaminols

Siderophore Receptor-Mediated Uptake of Lactivicin Analogues in Gram-Negative Bacteria

Selective Targeting of Bromodomains of the Bromodomain-PHD Fingers Family Impairs Osteoclast Differentiation

A direct copper-catalyzed route to pyrrolo-fused heterocycles from boronic acids

Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841)

Pyridone-Conjugated Monobactam Antibiotics with Gram-Negative Activity

Diazonamide Support Studies: Stereoselective Formation of the C10 Chiral Center in both the CDEFG and AEFG Fragments

Novel monobactams utilizing a siderophore uptake mechanism for the treatment of gram-negative infections

Structural Characterization of an Enantiomerically Pure Amino Acid Imidazolide and Direct Formation of the β-Lactam Nucleus from an α-Amino Acid

Carbanion Stabilization by Distal Silyloxy Groups. Origin of the High Diastereoselectivity in the Formation of Quaternary Centers with Aryllead(IV) Triacetate Reagents

One-pot copper-catalyzed synthesis of N-functionalized pyrazoles from boronic acids

ChemInform Abstract: A Direct Copper-Catalyzed Route to Pyrrolo-Fused Heterocycles from Boronic Acids

Corrigendum to “Novel monobactams utilizing a siderophore uptake mechanism for the treatment of Gram-negative infections” [Bioorg. Med. Chem. Lett. 22/18 (2012) 5989–5994]

tert-Buyldiphenylsilylethyl (“TBDPSE”): A Practical Protecting Group for Phenols

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