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The Discovery of 7‑Methyl-2-[(7-methyl[1,2,4]triazolo[1,5‑a]pyridin-6-yl)amino]-9-(tetrahydro‑2H‑pyran-4-yl)-7,9-dihydro‑8H‑purin-8-one (AZD7648), a Potent and Selective DNA-Dependent Protein Kinase (DNA-PK) Inhibitor

Journal of medicinal chemistry, 2020-04, Vol.63 (7), p.3461-3471

2020

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Discovery of Clinical Candidate AZD0095, a Selective Inhibitor of Monocarboxylate Transporter 4 (MCT4) for Oncology

Journal of medicinal chemistry, 2023-01, Vol.66 (1), p.384-397

2023

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Direct targeting of FOXP3 in Tregs with AZD8701, a novel antisense oligonucleotide to relieve immunosuppression in cancer

Journal for immunotherapy of cancer, 2022-04, Vol.10 (4), p.e003892

2022

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Asymmetric synthesis of 2-alkyl-substituted tetrahydroquinolines by an enantioselective aza-Michael reaction

Organic & biomolecular chemistry, 2012-06, Vol.10 (22), p.4424-4432

2012

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General synthetic strategies towards N-alkyl sulfoximine building blocks for medicinal chemistry and the use of dimethylsulfoximine as a versatile precursor

Tetrahedron, 2014-09, Vol.70 (37), p.6613-6622

2014

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Designing novel building blocks is an overlooked strategy to improve compound quality

Drug discovery today, 2015-01, Vol.20 (1), p.11-17

2015

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Medicinal Chemistry of Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1)

Journal of medicinal chemistry, 2014-06, Vol.57 (11), p.4466-4486

2014

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α‐Functionalisation of Cyclic Sulfides Enabled by Lithiation Trapping

Angewandte Chemie International Edition, 2024-01, Vol.63 (2), p.e202314423-n/a

International ed. in English, 2024

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The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5- a ]pyridin-6-yl)amino]-9-(tetrahydro-2 H -pyran-4-yl)-7,9-dihydro-8 H -purin-8-one (AZD7648), a Potent and Selective DNA-Dependent Protein Kinase (DNA-PK) Inhibitor

Journal of medicinal chemistry, 2020-04, Vol.63 (7), p.3461-3471

2020

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Evolution of Small Molecule Kinase Drugs

ACS medicinal chemistry letters, 2019-02, Vol.10 (2), p.153-160

2019

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Preclinical Evaluation of AZ12601011 and AZ12799734, Inhibitors of Transforming Growth Factor β Superfamily Type 1 Receptors

Molecular pharmacology, 2019-02, Vol.95 (2), p.222-234

2019

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Chemical Biology Approaches Confirm MCT4 as the Therapeutic Target of a Cellular Optimized Hit

ACS chemical biology, 2023-02, Vol.18 (2), p.296-303

2023

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Optimization of a series of novel, potent and selective Macrocyclic SYK inhibitors

Bioorganic & medicinal chemistry letters, 2023-07, Vol.91, p.129352-129352, Article 129352

2023

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Discovery of AZD4747, a Potent and Selective Inhibitor of Mutant GTPase KRAS G12C with Demonstrable CNS Penetration

Journal of medicinal chemistry, 2023-07, Vol.66 (13), p.9147-9160

2023

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α‐Functionalisation of Cyclic Sulfides Enabled by Lithiation Trapping

Angewandte Chemie, 2024-01, Vol.136 (2), p.n/a

2024

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Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRAS G12C

Journal of medicinal chemistry, 2022-05, Vol.65 (9), p.6940-6952

2022

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Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRASG12C

Journal of medicinal chemistry, 2022-05, Vol.65 (9), p.6940-6952

2022

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Optimization of a series of potent, selective and orally bioavailable SYK inhibitors

Bioorganic & medicinal chemistry letters, 2020-10, Vol.30 (19), p.127433, Article 127433

2020

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Optimization of hERG and Pharmacokinetic Properties for Basic Dihydro‑8H‑purin-8-one Inhibitors of DNA-PK

ACS medicinal chemistry letters, 2022-08, Vol.13 (8), p.1295-1301

2022

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An Expedient Formal Total Synthesis of (−)-Diazonamide A via a Powerful, Stereoselective O-Aryl to C-Aryl Migration To Form the C10 Quaternary Center

Journal of the American Chemical Society, 2007-10, Vol.129 (40), p.12320-12327

2007

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Optimization of hERG and Pharmacokinetic Properties for Basic Dihydro-8 H -purin-8-one Inhibitors of DNA-PK

ACS medicinal chemistry letters, 2022-08, Vol.13 (8), p.1295-1301

2022

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Free-Wilson and Structural Approaches to Co-optimizing Human and Rodent Isoform Potency for 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitors

Journal of medicinal chemistry, 2012-12, Vol.55 (23), p.10652-10661

2012

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Optimization of Brain Penetrant 11β-Hydroxysteroid Dehydrogenase Type I Inhibitors and in Vivo Testing in Diet-Induced Obese Mice

Journal of medicinal chemistry, 2014-02, Vol.57 (3), p.970-986

2014

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Optimized scale up of 3-pyrimidinylpyrazolo[1,5-a]pyridine via Suzuki coupling; a general method of accessing a range of 3-(hetero)arylpyrazolo[1,5-a]pyridines

Tetrahedron, 2012-07, Vol.68 (27-28), p.5434-5444

2012

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The Discovery of 7‑Methyl-2-[(7-methyl[1,2,4]triazolo[1,5‑a]pyridin-6-yl)amino]-9-(tetrahydro‑2H‑pyran-4-yl)-7,9-dihydro‑8H‑purin-8-one (AZD7648), a Potent and Selective DNA-Dependent Protein Kinase (DNA-PK) Inhibitor

Discovery of Clinical Candidate AZD0095, a Selective Inhibitor of Monocarboxylate Transporter 4 (MCT4) for Oncology

Direct targeting of FOXP3 in Tregs with AZD8701, a novel antisense oligonucleotide to relieve immunosuppression in cancer

Asymmetric synthesis of 2-alkyl-substituted tetrahydroquinolines by an enantioselective aza-Michael reaction

General synthetic strategies towards N-alkyl sulfoximine building blocks for medicinal chemistry and the use of dimethylsulfoximine as a versatile precursor

Designing novel building blocks is an overlooked strategy to improve compound quality

Medicinal Chemistry of Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1)

α‐Functionalisation of Cyclic Sulfides Enabled by Lithiation Trapping

The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5- a ]pyridin-6-yl)amino]-9-(tetrahydro-2 H -pyran-4-yl)-7,9-dihydro-8 H -purin-8-one (AZD7648), a Potent and Selective DNA-Dependent Protein Kinase (DNA-PK) Inhibitor

Evolution of Small Molecule Kinase Drugs

Preclinical Evaluation of AZ12601011 and AZ12799734, Inhibitors of Transforming Growth Factor β Superfamily Type 1 Receptors

Chemical Biology Approaches Confirm MCT4 as the Therapeutic Target of a Cellular Optimized Hit

Optimization of a series of novel, potent and selective Macrocyclic SYK inhibitors

Discovery of AZD4747, a Potent and Selective Inhibitor of Mutant GTPase KRAS G12C with Demonstrable CNS Penetration

α‐Functionalisation of Cyclic Sulfides Enabled by Lithiation Trapping

Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRAS G12C

Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRASG12C

Optimization of a series of potent, selective and orally bioavailable SYK inhibitors

Optimization of hERG and Pharmacokinetic Properties for Basic Dihydro‑8H‑purin-8-one Inhibitors of DNA-PK

An Expedient Formal Total Synthesis of (−)-Diazonamide A via a Powerful, Stereoselective O-Aryl to C-Aryl Migration To Form the C10 Quaternary Center

Optimization of hERG and Pharmacokinetic Properties for Basic Dihydro-8 H -purin-8-one Inhibitors of DNA-PK

Structure-Based Design and Pharmacokinetic Optimization of Covalent Allosteric Inhibitors of the Mutant GTPase KRAS G12C

Free-Wilson and Structural Approaches to Co-optimizing Human and Rodent Isoform Potency for 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitors

Optimization of Brain Penetrant 11β-Hydroxysteroid Dehydrogenase Type I Inhibitors and in Vivo Testing in Diet-Induced Obese Mice

Optimized scale up of 3-pyrimidinylpyrazolo[1,5-a]pyridine via Suzuki coupling; a general method of accessing a range of 3-(hetero)arylpyrazolo[1,5-a]pyridines

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