List of works - James S. Scott

A Buchwald-Hartwig Protocol to Enable Rapid Linker Exploration of Cereblon E3-Ligase PROTACs

scientific article published on 24 July 2020

A new series of neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase

scientific article published on 21 November 2007

Addition of Fluorine and a Late-Stage Functionalization (LSF) of the Oral SERD AZD9833

scientific article published on 28 October 2020

An Umpolung Approach to Alkene Carboamination: Palladium Catalyzed 1,2-Amino-Acylation, -Carboxylation, -Arylation, -Vinylation, and -Alkynylation

scientific article published on 28 May 2015

Building Bridges in a Series of Estrogen Receptor Degraders: An Application of Metathesis in Medicinal Chemistry

scientific article published on 23 September 2019

Circumventing seizure activity in a series of G protein coupled receptor 119 (GPR119) agonists.

scientific article published on 3 November 2014

Clean six-step synthesis of a piperidino-thiomorpholine library using polymer-supported reagents

article

Clean synthesis of α-bromo ketones and their utilisation in the synthesis of 2-alkoxy-2,3-dihydro-2-aryl-1,4-benzodioxanes, 2-amino-4-aryl-1,3-thiazoles and piperidino-2-amino-1,3-thiazoles using polymer-supported reagents

article published in 1999

Conformational restriction in a series of GPR119 agonists: differences in pharmacology between mouse and human

scientific article published on 10 April 2013

Correction to Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators

scientific article published on 22 March 2016

Development of a practical Buchwald-Hartwig amine arylation protocol using a conveniently prepared (NHC)Pd(R-allyl)Cl catalyst

scientific article published on 6 June 2008

Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88L265P Diffuse Large B-Cell Lymphoma

scientific article published on 27 November 2017

Discovery of AZD9833, a potent and orally bioavailable selective estrogen receptor degrader and antagonist

scientific article published on 10 September 2020

Discovery of a Potent, Selective, and Orally Bioavailable Acidic 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitor: Discovery of 2-[(3S)-1-[5-(Cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic Acid (AZD4017) ⬇️

scientific article published on June 19, 2012

Discovery of a Series of 5-Azaquinazolines as Orally Efficacious IRAK4 Inhibitors Targeting MyD88L265P Mutant Diffuse Large B Cell Lymphoma

scientific article published on 01 November 2019

Discovery, optimisation and in vivo evaluation of novel GPR119 agonists.

scientific article published on 18 October 2011

Enantioselective Narasaka-Heck cyclizations: synthesis of tetrasubstituted nitrogen-bearing stereocenters

scientific article published on 24 November 2016

Free-Wilson and structural approaches to co-optimizing human and rodent isoform potency for 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors

scientific article

Highly selective entry to the azadirachtin skeleton via a Claisen rearrangement/radical cyclization sequence.

scientific article published in October 2002

Improving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors

scientific article published on 15 October 2020

Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators

scientific article

Lipophilicity trends upon fluorination of isopropyl, cyclopropyl and 3-oxetanyl groups

scientific article published on 02 September 2020

Lowering Lipophilicity by Adding Carbon: AzaSpiroHeptanes, a logD Lowering Twist

scientific article published on 18 July 2019

Lowering Lipophilicity by Adding Carbon: One-Carbon Bridges of Morpholines and Piperazines

scientific article published on 20 September 2018

Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1).

scientific article published on 13 December 2013

Multi-step organic synthesis using solid-supported reagents and scavengers: a new paradigm in chemical library generation

article

Neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.

scientific article published on 2 September 2007

Novel Acidic 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitor with Reduced Acyl Glucuronide Liability: The Discovery of 4-[4-(2-Adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic Acid (AZD8329) ⬇️

scientific article published on November 7, 2012

Optimisation of pharmacokinetic properties in a neutral series of 11β-HSD1 inhibitors ⬇️

scientific article published on 05 September 2012

Optimization of brain penetrant 11β-hydroxysteroid dehydrogenase type I inhibitors and in vivo testing in diet-induced obese mice

scientific article

Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4.

scientific article

Palladium catalyzed cyclizations of oximeesters with 1,1-disubstituted alkenes: synthesis of α,α-disubstituted dihydropyrroles and studies towards an asymmetric protocol ⬇️

scientific article published on February 21, 2013

Pd-Catalyzed C-H aziridination of 3,3,5,5-tetrasubstituted piperazin-2-ones

scientific article

Potent and Selective Inhibitors of MTH1 Probe Its Role in Cancer Cell Survival

scientific article

Practical application of ligand efficiency metrics in lead optimisation

scientific article published on 05 April 2018

Reducing the lipophilicity of perfluoroalkyl groups by CF2-F/CF2-Me or CF3/CH3 exchange

scientific article published on 28 November 2018

Skipped Fluorination Motifs: Synthesis of Building Blocks and Comparison of Lipophilicity Trends with Vicinal and Isolated Fluorination Motifs

scientific article published on 05 January 2021

Structure-Guided Design and In-Cell Target Profiling of a Cell-Active Target Engagement Probe for PARP Inhibitors

scientific article published on 10 February 2020

Sustained wash-resistant receptor activation responses of GPR119 agonists

scientific article published on 19 June 2015

Synthesis of the potent analgesic compound (±)-epibatidine using an orchestrated multi-step sequence of polymer supported reagents

article

Systematic Investigation of Lipophilicity Modulation by Aliphatic Fluorination Motifs

scientific article published on 17 January 2020

Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat.

scientific article published on 19 December 2015

The synthesis of azadirachtin: a potent insect antifeedant.

scientific article published in January 2008

Total Synthesis of Rapamycin

scientific article published on 01 January 2007

Total synthesis of rapamycin

scientific article published in January 2009

Tricyclic Indazoles-A Novel Class of Selective Estrogen Receptor Degrader Antagonists

scientific article published on 30 January 2019

Use of small-molecule crystal structures to address solubility in a novel series of G protein coupled receptor 119 agonists: optimization of a lead and in vivo evaluation.

scientific article

List of works by James S. Scott

A Buchwald-Hartwig Protocol to Enable Rapid Linker Exploration of Cereblon E3-Ligase PROTACs

A new series of neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase

Addition of Fluorine and a Late-Stage Functionalization (LSF) of the Oral SERD AZD9833

An Umpolung Approach to Alkene Carboamination: Palladium Catalyzed 1,2-Amino-Acylation, -Carboxylation, -Arylation, -Vinylation, and -Alkynylation

Building Bridges in a Series of Estrogen Receptor Degraders: An Application of Metathesis in Medicinal Chemistry

Circumventing seizure activity in a series of G protein coupled receptor 119 (GPR119) agonists.

Clean six-step synthesis of a piperidino-thiomorpholine library using polymer-supported reagents

Clean synthesis of α-bromo ketones and their utilisation in the synthesis of 2-alkoxy-2,3-dihydro-2-aryl-1,4-benzodioxanes, 2-amino-4-aryl-1,3-thiazoles and piperidino-2-amino-1,3-thiazoles using polymer-supported reagents

Conformational restriction in a series of GPR119 agonists: differences in pharmacology between mouse and human

Correction to Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators

Development of a practical Buchwald-Hartwig amine arylation protocol using a conveniently prepared (NHC)Pd(R-allyl)Cl catalyst

Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88L265P Diffuse Large B-Cell Lymphoma

Discovery of AZD9833, a potent and orally bioavailable selective estrogen receptor degrader and antagonist

Discovery of a Potent, Selective, and Orally Bioavailable Acidic 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitor: Discovery of 2-[(3S)-1-[5-(Cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic Acid (AZD4017) ⬇️

Discovery of a Series of 5-Azaquinazolines as Orally Efficacious IRAK4 Inhibitors Targeting MyD88L265P Mutant Diffuse Large B Cell Lymphoma

Discovery, optimisation and in vivo evaluation of novel GPR119 agonists.

Enantioselective Narasaka-Heck cyclizations: synthesis of tetrasubstituted nitrogen-bearing stereocenters

Free-Wilson and structural approaches to co-optimizing human and rodent isoform potency for 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors

Highly selective entry to the azadirachtin skeleton via a Claisen rearrangement/radical cyclization sequence.

Improving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors

Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators

Lipophilicity trends upon fluorination of isopropyl, cyclopropyl and 3-oxetanyl groups

Lowering Lipophilicity by Adding Carbon: AzaSpiroHeptanes, a logD Lowering Twist

Lowering Lipophilicity by Adding Carbon: One-Carbon Bridges of Morpholines and Piperazines

Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1).

Multi-step organic synthesis using solid-supported reagents and scavengers: a new paradigm in chemical library generation

Neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.

Novel Acidic 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitor with Reduced Acyl Glucuronide Liability: The Discovery of 4-[4-(2-Adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic Acid (AZD8329) ⬇️

Optimisation of pharmacokinetic properties in a neutral series of 11β-HSD1 inhibitors ⬇️

Optimization of brain penetrant 11β-hydroxysteroid dehydrogenase type I inhibitors and in vivo testing in diet-induced obese mice

Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4.

Palladium catalyzed cyclizations of oximeesters with 1,1-disubstituted alkenes: synthesis of α,α-disubstituted dihydropyrroles and studies towards an asymmetric protocol ⬇️

Pd-Catalyzed C-H aziridination of 3,3,5,5-tetrasubstituted piperazin-2-ones

Potent and Selective Inhibitors of MTH1 Probe Its Role in Cancer Cell Survival

Practical application of ligand efficiency metrics in lead optimisation

Reducing the lipophilicity of perfluoroalkyl groups by CF2-F/CF2-Me or CF3/CH3 exchange

Skipped Fluorination Motifs: Synthesis of Building Blocks and Comparison of Lipophilicity Trends with Vicinal and Isolated Fluorination Motifs

Structure-Guided Design and In-Cell Target Profiling of a Cell-Active Target Engagement Probe for PARP Inhibitors

Sustained wash-resistant receptor activation responses of GPR119 agonists

Synthesis of the potent analgesic compound (±)-epibatidine using an orchestrated multi-step sequence of polymer supported reagents

Systematic Investigation of Lipophilicity Modulation by Aliphatic Fluorination Motifs

Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat.

The synthesis of azadirachtin: a potent insect antifeedant.

Total Synthesis of Rapamycin

Total synthesis of rapamycin

Tricyclic Indazoles-A Novel Class of Selective Estrogen Receptor Degrader Antagonists

Use of small-molecule crystal structures to address solubility in a novel series of G protein coupled receptor 119 agonists: optimization of a lead and in vivo evaluation.