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Minisci reactions: Versatile CH-functionalizations for medicinal chemists

MedChemComm, 2011-12, Vol.2 (12), p.1135-1161

Duncton, Matthew A. J

2011

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A New Drug Discovery Platform: Application to DNA Polymerase Eta and Apurinic/Apyrimidinic Endonuclease 1

International journal of molecular sciences, 2023-12, Vol.24 (23), p.16637

2023

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Orally Absorbed Derivatives of the β‑Lactamase Inhibitor Avibactam. Design of Novel Prodrugs of Sulfate Containing Drugs

Journal of medicinal chemistry, 2018-11, Vol.61 (22), p.10340-10344

2018

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Tetrazolone as an acid bioisostere: application to marketed drugs containing a carboxylic acid

Organic & biomolecular chemistry, 2016-01, Vol.14 (39), p.9343-9347

2016

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Preparation of Heteroaryloxetanes and Heteroarylazetidines by Use of a Minisci Reaction

Journal of organic chemistry, 2009-08, Vol.74 (16), p.6354-6357

2009

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Synthesis of trans-2-(Trifluoromethyl)cyclopropanes via Suzuki Reactions with an N‑Methyliminodiacetic Acid Boronate

Organic letters, 2013-09, Vol.15 (17), p.4284-4287

2013

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Preparation of Aryloxetanes and Arylazetidines by Use of an Alkyl−Aryl Suzuki Coupling

Organic letters, 2008-08, Vol.10 (15), p.3259-3262

2008

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5-Benzyloxytryptamine as an antagonist of TRPM8

Bioorganic & medicinal chemistry letters, 2010-12, Vol.20 (23), p.7076-7079

2010

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Development of a MEK inhibitor, NFX-179, as a chemoprevention agent for squamous cell carcinoma

Science translational medicine, 2023-10, Vol.15 (717), p.eade1844

2023

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Early Drug Discovery and Development of Novel Cancer Therapeutics Targeting DNA Polymerase Eta (POLH)

Frontiers in oncology, 2021-11, Vol.11, p.778925-778925

2021

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Toward Orally Absorbed Prodrugs of the Antibiotic Aztreonam. Design of Novel Prodrugs of Sulfate Containing Drugs. Part 2

ACS medicinal chemistry letters, 2020-02, Vol.11 (2), p.162-165

2020

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A one-pot synthesis of tetrazolones from acid chlorides: understanding functional group compatibility, and application to the late-stage functionalization of marketed drugs

Organic & biomolecular chemistry, 2016-01, Vol.14 (39), p.9338-9342

2016

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Enantioselective synthesis of an octahydroindolizine (indolizidine) alcohol using an enzymatic resolution

Organic & biomolecular chemistry, 2017-04, Vol.15 (14), p.2953-2961

2017

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TRPV4 agonists and antagonists

Current topics in medicinal chemistry, 2011-09, Vol.11 (17), p.2216

2011

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A Single-Step Synthesis of Azetidine-3-amines

Journal of organic chemistry, 2020-10, Vol.85 (20), p.13317-13323

2020

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Novel tricyclic azepine derivatives: Biological evaluation of pyrimido[4,5- b]-1,4-benzoxazepines, thiazepines, and diazepines as inhibitors of the epidermal growth factor receptor tyrosine kinase

Bioorganic & medicinal chemistry letters, 2006-10, Vol.16 (19), p.5102-5106

2006

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A concise one-pot synthesis of trifluoromethyl-containing 2,6-disubstituted 5,6,7,8-tetrahydroquinolines and 5,6,7,8-tetrahydronaphthyridines

Organic & biomolecular chemistry, 2013-02, Vol.11 (8), p.1358-1366

2013

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Identification and characterization of novel TRPV4 modulators

Biochemical and biophysical research communications, 2009-11, Vol.389 (3), p.490-494

2009

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Fragment- and structure-based drug discovery for developing therapeutic agents targeting the DNA Damage Response

Progress in biophysics and molecular biology, 2021-08, Vol.163, p.130-142

2021

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Arylphthalazines as potent, and orally bioavailable inhibitors of VEGFR-2

Bioorganic & medicinal chemistry, 2009-01, Vol.17 (2), p.731-740

2009

Volltextzugriff (PDF)

Tuning the Reactivity of Nuclear Factor Erythroid 2‑Related Factor 2 (Nrf2) Activators for Optimal in Vivo Efficacy

ACS medicinal chemistry letters, 2023-12, Vol.14 (12), p.1700-1706

2023

Volltextzugriff (PDF)

Mining biologically-active molecules for inhibitors of fatty acid amide hydrolase (FAAH): Identification of phenmedipham and amperozide as FAAH inhibitors

Bioorganic & medicinal chemistry letters, 2009-12, Vol.19 (23), p.6793-6796

2009

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Identification of orally-bioavailable antagonists of the TRPV4 ion-channel

Bioorganic & medicinal chemistry letters, 2015-09, Vol.25 (18), p.4011-4015

2015

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Preparation of Substituted Pyrimido[4,5-b]-1,4-benzoxazepines, Thiazepines, and Diazepines via a Pictet−Spengler Cyclization

Journal of organic chemistry, 2005-11, Vol.70 (23), p.9629-9631

2005

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TRPM8 biology and medicinal chemistry

Current topics in medicinal chemistry, 2011-09, Vol.11 (17), p.2237

2011

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Minisci reactions: Versatile CH-functionalizations for medicinal chemists

A New Drug Discovery Platform: Application to DNA Polymerase Eta and Apurinic/Apyrimidinic Endonuclease 1

Orally Absorbed Derivatives of the β‑Lactamase Inhibitor Avibactam. Design of Novel Prodrugs of Sulfate Containing Drugs

Tetrazolone as an acid bioisostere: application to marketed drugs containing a carboxylic acid

Preparation of Heteroaryloxetanes and Heteroarylazetidines by Use of a Minisci Reaction

Synthesis of trans-2-(Trifluoromethyl)cyclopropanes via Suzuki Reactions with an N‑Methyliminodiacetic Acid Boronate

Preparation of Aryloxetanes and Arylazetidines by Use of an Alkyl−Aryl Suzuki Coupling

5-Benzyloxytryptamine as an antagonist of TRPM8

Development of a MEK inhibitor, NFX-179, as a chemoprevention agent for squamous cell carcinoma

Early Drug Discovery and Development of Novel Cancer Therapeutics Targeting DNA Polymerase Eta (POLH)

Toward Orally Absorbed Prodrugs of the Antibiotic Aztreonam. Design of Novel Prodrugs of Sulfate Containing Drugs. Part 2

A one-pot synthesis of tetrazolones from acid chlorides: understanding functional group compatibility, and application to the late-stage functionalization of marketed drugs

Enantioselective synthesis of an octahydroindolizine (indolizidine) alcohol using an enzymatic resolution

TRPV4 agonists and antagonists

A Single-Step Synthesis of Azetidine-3-amines

Novel tricyclic azepine derivatives: Biological evaluation of pyrimido[4,5- b]-1,4-benzoxazepines, thiazepines, and diazepines as inhibitors of the epidermal growth factor receptor tyrosine kinase

A concise one-pot synthesis of trifluoromethyl-containing 2,6-disubstituted 5,6,7,8-tetrahydroquinolines and 5,6,7,8-tetrahydronaphthyridines

Identification and characterization of novel TRPV4 modulators

Fragment- and structure-based drug discovery for developing therapeutic agents targeting the DNA Damage Response

Arylphthalazines as potent, and orally bioavailable inhibitors of VEGFR-2

Tuning the Reactivity of Nuclear Factor Erythroid 2‑Related Factor 2 (Nrf2) Activators for Optimal in Vivo Efficacy

Mining biologically-active molecules for inhibitors of fatty acid amide hydrolase (FAAH): Identification of phenmedipham and amperozide as FAAH inhibitors

Identification of orally-bioavailable antagonists of the TRPV4 ion-channel

Preparation of Substituted Pyrimido[4,5-b]-1,4-benzoxazepines, Thiazepines, and Diazepines via a Pictet−Spengler Cyclization

TRPM8 biology and medicinal chemistry

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