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Identification of (R)‑N‑((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)‑1H‑indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B‑Cell Lymphomas

Journal of medicinal chemistry, 2016-11, Vol.59 (21), p.9928-9941

2016

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Largazole and its derivatives selectively inhibit ubiquitin activating enzyme (e1)

PloS one, 2012-01, Vol.7 (1), p.e29208

2012

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A Concise Total Synthesis of Largazole, Solution Structure, and Some Preliminary Structure Activity Relationships

Organic letters, 2008-08, Vol.10 (16), p.3595-3598

2008

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Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance

Bioorganic & medicinal chemistry letters, 2017-08, Vol.27 (15), p.3534-3541

2017

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Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2

ACS medicinal chemistry letters, 2014-04, Vol.5 (4), p.378-383

2014

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Identification and mechanistic studies of a novel ubiquitin E1 inhibitor

Journal of biomolecular screening, 2012-04, Vol.17 (4), p.421-434

2012

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Discovery of Benzotriazolo[4,3‑d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains

ACS medicinal chemistry letters, 2016-02, Vol.7 (2), p.145-150

2016

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A Diastereoselective Ring Contraction of 1,3-Dioxepins to 2,3,4-Trisubstituted and Tetrasubstituted Tetrahydrofurans

Journal of organic chemistry, 2008-01, Vol.73 (2), p.612-617

2008

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Structural Characterization of Degrader-Induced Ternary Complexes Using Hydrogen–Deuterium Exchange Mass Spectrometry and Computational Modeling: Implications for Structure-Based Design

ACS chemical biology, 2021-11, Vol.16 (11), p.2228-2243

2021

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Regioselective Lewis Acid-Mediated [1,3] Rearrangement of Allylvinyl Ethers

Organic letters, 2005-05, Vol.7 (11), p.2173-2176

2005

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The [1, 3] O-to-C rearrangement: opportunities for stereoselective synthesis

Organic & biomolecular chemistry, 2008-01, Vol.6 (2), p.240-254

2008

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Evaluation of the Small-molecule BRD4 Degrader CFT-2718 in Small-cell Lung Cancer and Pancreatic Cancer Models

Molecular cancer therapeutics, 2021-08, Vol.20 (8), p.1367-1377

2021

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Preclinical Development of the Class-I-Selective Histone Deacetylase Inhibitor OKI-179 for the Treatment of Solid Tumors

Molecular cancer therapeutics, 2022-03, Vol.21 (3), p.397-406

2022

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Discovery, design, and synthesis of indole-based EZH2 inhibitors

Bioorganic & medicinal chemistry letters, 2015-09, Vol.25 (17), p.3644-3649

2015

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A modular approach to the synthesis of 2,3,4-trisubstituted tetrahydrofurans

Chemical communications (Cambridge, England), 2006-01 (29), p.3119-3121

2006

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A Practical Synthesis of Indoles via a Pd-Catalyzed C–N Ring Formation

Organic letters, 2014-08, Vol.16 (16), p.4114-4117

2014

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Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors

ACS medicinal chemistry letters, 2013-09, Vol.4 (9), p.835-840

2013

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Development of methyl isoxazoleazepines as inhibitors of BET

Bioorganic & medicinal chemistry letters, 2015-05, Vol.25 (9), p.1842-1848

2015

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A Method for Determining the Kinetics of Small-Molecule-Induced Ubiquitination

SLAS discovery, 2021-04, Vol.26 (4), p.547-559

2021

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Stereoselective Lewis Acid Mediated [1,3] Ring Contraction of 2,5-Dihydrooxepins as a Route to Polysubstituted Cyclopentenes

Angewandte Chemie (International ed.), 2005-05, Vol.44 (21), p.3264-3267

2005

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Largazole and its derivatives selectively inhibit ubiquitin activating enzyme (e1)

A Concise Total Synthesis of Largazole, Solution Structure, and Some Preliminary Structure Activity Relationships

Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance

Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2

Identification and mechanistic studies of a novel ubiquitin E1 inhibitor

Discovery of Benzotriazolo[4,3‑d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains

Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials

A Diastereoselective Ring Contraction of 1,3-Dioxepins to 2,3,4-Trisubstituted and Tetrasubstituted Tetrahydrofurans

Structural Characterization of Degrader-Induced Ternary Complexes Using Hydrogen–Deuterium Exchange Mass Spectrometry and Computational Modeling: Implications for Structure-Based Design

Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains

Regioselective Lewis Acid-Mediated [1,3] Rearrangement of Allylvinyl Ethers

The [1, 3] O-to-C rearrangement: opportunities for stereoselective synthesis

Evaluation of the Small-molecule BRD4 Degrader CFT-2718 in Small-cell Lung Cancer and Pancreatic Cancer Models

Preclinical Development of the Class-I-Selective Histone Deacetylase Inhibitor OKI-179 for the Treatment of Solid Tumors

Discovery, design, and synthesis of indole-based EZH2 inhibitors

A modular approach to the synthesis of 2,3,4-trisubstituted tetrahydrofurans

A Practical Synthesis of Indoles via a Pd-Catalyzed C–N Ring Formation

GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1‑like

Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors

Development of methyl isoxazoleazepines as inhibitors of BET

EZH2 Inhibitor Efficacy in Non-Hodgkin’s Lymphoma Does Not Require Suppression of H3K27 Monomethylation

A Method for Determining the Kinetics of Small-Molecule-Induced Ubiquitination

Stereoselective Lewis Acid Mediated [1,3] Ring Contraction of 2,5-Dihydrooxepins as a Route to Polysubstituted Cyclopentenes

GNE-886: A Potent and Selective Inhibitor of the Cat Eye Syndrome Chromosome Region Candidate 2 Bromodomain (CECR2)

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