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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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AZD1208, a potent and selective pan-Pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemia

Blood, 2014-02, Vol.123 (6), p.905-913

2014

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Structure- and Reactivity-Based Development of Covalent Inhibitors of the Activating and Gatekeeper Mutant Forms of the Epidermal Growth Factor Receptor (EGFR)

Journal of medicinal chemistry, 2013-09, Vol.56 (17), p.7025-7048

2013

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

Journal of medicinal chemistry, 2016-06, Vol.59 (11), p.5391-5402

2016

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Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases

Bioorganic & medicinal chemistry letters, 2012-07, Vol.22 (14), p.4599-4604

2012

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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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[4 + 2]-Annulations of Chiral Organosilanes: Application to the Total Synthesis of Leucascandrolide A

Journal of organic chemistry, 2007-01, Vol.72 (1), p.2-24

2007

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Mitigation of cardiovascular toxicity in a series of CSF-1R inhibitors, and the identification of AZD7507

Bioorganic & medicinal chemistry letters, 2013-08, Vol.23 (16), p.4591-4596

2013

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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 of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases

Bioorganic & medicinal chemistry letters, 2018-05, Vol.28 (8), p.1336-1341

2018

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A Mild, Chemoselective Protocol for the Removal of Thioketals and Thioacetals Mediated by Dess−Martin Periodinane

Organic letters, 2003-02, Vol.5 (4), p.575-578

2003

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3-Amido-4-anilinocinnolines as a novel class of CSF-1R inhibitor

Bioorganic & medicinal chemistry letters, 2011-03, Vol.21 (5), p.1382-1384

2011

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Discovery of novel hedgehog antagonists from cell-based screening: Isosteric modification of p38 bisamides as potent inhibitors of SMO

Bioorganic & medicinal chemistry letters, 2012-07, Vol.22 (14), p.4907-4911

2012

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Synthesis of the C1‘−C11‘ Oxazole-Containing Side Chain of Leucascandrolide A. Application of a Sonogashira Cross-Coupling

Journal of organic chemistry, 2002-09, Vol.67 (19), p.6812-6815

2002

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Slow-Onset, Long-Duration, Alkyl Analogues of Methylphenidate with Enhanced Selectivity for the Dopamine Transporter

Journal of medicinal chemistry, 2007-01, Vol.50 (2), p.219-232

2007

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Enantioselective [4 + 2]-Annulation of Chiral Crotylsilanes: Application to the Synthesis of a C1−C22 Fragment of Leucascandrolide A

Organic letters, 2003-10, Vol.5 (21), p.3995-3998

2003

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Sonogashira Coupling of Functionalized Trifloyl Oxazoles and Thiazoles with Terminal Alkynes: Synthesis of Disubstituted Heterocycles

Organic letters, 2002-07, Vol.4 (15), p.2485-2488

2002

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3-Amido-4-anilinoquinolines as CSF-1R kinase inhibitors 2: Optimization of the PK profile

Bioorganic & medicinal chemistry letters, 2009-02, Vol.19 (3), p.701-705

2009

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Pyridyl and thiazolyl bisamide CSF-1R inhibitors for the treatment of cancer

Bioorganic & medicinal chemistry letters, 2008-09, Vol.18 (17), p.4794-4797

2008

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Speciation and Mechanistic Studies of Chiral Copper(I) Schiff Base Precursors Mediating Asymmetric Carbenoid Insertion Reactions of Diazoacetates into the Si−H Bond of Silanes

Organometallics, 2000-07, Vol.19 (15), p.2896-2908

2000

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Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity

Bioorganic & medicinal chemistry letters, 2009-02, Vol.19 (3), p.1026-1029

2009

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Vinylogous amide analogs of methylphenidate

Bioorganic & medicinal chemistry letters, 2005-06, Vol.15 (12), p.3044-3047

2005

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Heteroarylamide smoothened inhibitors: Discovery of N-[2,4-dimethyl-5-(1-methylimidazol-4-yl)phenyl]-4-(2-pyridylmethoxy)benzamide (AZD8542) and N-[5-(1H-imidazol-2-yl)-2,4-dimethyl-phenyl]-4-(2- pyridylmethoxy)benzamide (AZD7254)

Bioorganic & medicinal chemistry, 2020-01, Vol.28 (2), p.115227, Article 115227

2020

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Lewis Acid-Mediated Carbocyclization Reactions of Chiral (E)-Crotylsilanes

Journal of organic chemistry, 1997-12, Vol.62 (26), p.9335-9338

1997

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AZD1208, a potent and selective pan-Pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemia

Structure- and Reactivity-Based Development of Covalent Inhibitors of the Activating and Gatekeeper Mutant Forms of the Epidermal Growth Factor Receptor (EGFR)

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

Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases

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

[4 + 2]-Annulations of Chiral Organosilanes: Application to the Total Synthesis of Leucascandrolide A

Mitigation of cardiovascular toxicity in a series of CSF-1R inhibitors, and the identification of AZD7507

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

Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases

A Mild, Chemoselective Protocol for the Removal of Thioketals and Thioacetals Mediated by Dess−Martin Periodinane

3-Amido-4-anilinocinnolines as a novel class of CSF-1R inhibitor

Discovery of novel hedgehog antagonists from cell-based screening: Isosteric modification of p38 bisamides as potent inhibitors of SMO

Synthesis of the C1‘−C11‘ Oxazole-Containing Side Chain of Leucascandrolide A. Application of a Sonogashira Cross-Coupling

Slow-Onset, Long-Duration, Alkyl Analogues of Methylphenidate with Enhanced Selectivity for the Dopamine Transporter

Enantioselective [4 + 2]-Annulation of Chiral Crotylsilanes: Application to the Synthesis of a C1−C22 Fragment of Leucascandrolide A

Sonogashira Coupling of Functionalized Trifloyl Oxazoles and Thiazoles with Terminal Alkynes: Synthesis of Disubstituted Heterocycles

3-Amido-4-anilinoquinolines as CSF-1R kinase inhibitors 2: Optimization of the PK profile

Pyridyl and thiazolyl bisamide CSF-1R inhibitors for the treatment of cancer

Speciation and Mechanistic Studies of Chiral Copper(I) Schiff Base Precursors Mediating Asymmetric Carbenoid Insertion Reactions of Diazoacetates into the Si−H Bond of Silanes

Identification of amidoheteroaryls as potent inhibitors of mutant (V600E) B-Raf kinase with in vivo activity

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

Vinylogous amide analogs of methylphenidate

Heteroarylamide smoothened inhibitors: Discovery of N-[2,4-dimethyl-5-(1-methylimidazol-4-yl)phenyl]-4-(2-pyridylmethoxy)benzamide (AZD8542) and N-[5-(1H-imidazol-2-yl)-2,4-dimethyl-phenyl]-4-(2- pyridylmethoxy)benzamide (AZD7254)

Lewis Acid-Mediated Carbocyclization Reactions of Chiral (E)-Crotylsilanes

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