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Acid-Mediated Ring Expansion of 2,2-Disubstituted Azetidine Carbamates to 6,6-Disubstituted 1,3-Oxazinan-2-ones

Organic letters, 2019-03, Vol.21 (6), p.1818-1822

2019

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A small molecule inhibitor of HER3: a proof-of-concept study

Biochemical journal, 2020-09, Vol.477 (17), p.3329-3347

2020

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Demonstration of the utility of DOS-derived fragment libraries for rapid hit derivatisation in a multidirectional fashion

Chemical science (Cambridge), 2020-10, Vol.11 (39), p.1792-181

2020

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Use of the Intramolecular Heck Reaction for Forming Congested Quaternary Carbon Stereocenters. Stereocontrolled Total Synthesis of (±)-Gelsemine

Journal of the American Chemical Society, 2005-12, Vol.127 (51), p.18054-18065

2005

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Tool inhibitors and assays to interrogate the biology of the TRAF2 and NCK interacting kinase

Bioorganic & medicinal chemistry letters, 2019-08, Vol.29 (15), p.1962-1967

2019

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Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition

Communications biology, 2020-12, Vol.3 (1), p.782-782, Article 782

2020

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Aza-Cope Rearrangement−Mannich Cyclizations for the Formation of Complex Tricyclic Amines: Stereocontrolled Total Synthesis of (±)-Gelsemine

Journal of the American Chemical Society, 2005-12, Vol.127 (51), p.18046-18053

2005

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High Fidelity Suzuki–Miyaura Coupling for the Synthesis of DNA Encoded Libraries Enabled by Micelle Forming Surfactants

Bioconjugate chemistry, 2020-01, Vol.31 (1), p.149-155

2020

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Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}- N -methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs

Journal of medicinal chemistry, 2021-10, Vol.64 (19), p.14498-14512

2021

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Functional Group Tolerance of a Micellar on-DNA Suzuki–Miyaura Cross-Coupling Reaction for DNA-Encoded Library Design

Journal of organic chemistry, 2021-12, Vol.86 (24), p.17930-17935

2021

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Screening Ultra-Large Encoded Compound Libraries Leads to Novel Protein–Ligand Interactions and High Selectivity

Journal of medicinal chemistry, 2024-01, Vol.67 (2), p.864-884

2024

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Scope of on-DNA nucleophilic aromatic substitution on weakly-activated heterocyclic substrates for the synthesis of DNA-encoded libraries

Bioorganic & medicinal chemistry, 2022-06, Vol.63, p.116688-116688, Article 116688

2022

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Synthesis of Structurally Diverse N‐Substituted Quaternary‐Carbon‐Containing Small Molecules from α,α‐Disubstituted Propargyl Amino Esters

Chemistry : a European journal, 2018-09, Vol.24 (51), p.13681-13687

2018

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Partially Saturated Bicyclic Heteroaromatics as an sp(3) -Enriched Fragment Collection

Angewandte Chemie International Edition, 2016-09, Vol.55 (40), p.12479-12483

2016

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Highly efficient on-DNA amide couplings promoted by micelle forming surfactants for the synthesis of DNA encoded libraries

Chemical science (Cambridge), 2021-07, Vol.12 (27), p.9475-9484

2021

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Discovery of a selective c-MET inhibitor with a novel binding mode

Bioorganic & medicinal chemistry letters, 2022-11, Vol.75, p.128948-128948, Article 128948

2022

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AiZynth impact on medicinal chemistry practice at AstraZeneca

RSC medicinal chemistry, 2024-04, Vol.15 (4), p.185-195

2024

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Abstract 296: Structure-based and property-based drug design of AZD5305, a highly selective PARP1 inhibitor and trapper

Cancer research (Chicago, Ill.), 2021-07, Vol.81 (13_Supplement), p.296-296

2021

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Discovery of 5‑{4-[(7-Ethyl-6-oxo‑5,6-dihydro‑1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}‑N‑methylpyridine-2-carboxamide (AZD5305): A PARP1–DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs

Journal of medicinal chemistry, 2021-10, Vol.64 (19), p.14498-14512

2021

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Discovery of Spiro-azaindoline Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1)

ACS medicinal chemistry letters, 2022-01, Vol.13 (1), p.84-91

2022

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Partially Saturated Bicyclic Heteroaromatics as an sp 3 ‐Enriched Fragment Collection

Angewandte Chemie International Edition, 2016-09, Vol.55 (40), p.12479-12483

2016

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Controlling stereoselection in intramolecular heck reactions by tailoring the palladium catalyst

Tetrahedron letters, 1992-08, Vol.33 (34), p.4859-4862

1992

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Partially Saturated Bicyclic Heteroaromatics as an sp3-Enriched Fragment Collection

Angewandte Chemie International Edition, 2016-09, Vol.55 (40), p.12479-12483

International ed. in English, 2016

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Identification and optimisation of a series of tetrahydrobenzotriazoles as metabotropic glutamate receptor 5-selective positive allosteric modulators that improve performance in a preclinical model of cognition

Bioorganic & medicinal chemistry letters, 2015-12, Vol.25 (24), p.5792-5796

2015

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Acid-Mediated Ring Expansion of 2,2-Disubstituted Azetidine Carbamates to 6,6-Disubstituted 1,3-Oxazinan-2-ones

A small molecule inhibitor of HER3: a proof-of-concept study

Demonstration of the utility of DOS-derived fragment libraries for rapid hit derivatisation in a multidirectional fashion

Use of the Intramolecular Heck Reaction for Forming Congested Quaternary Carbon Stereocenters. Stereocontrolled Total Synthesis of (±)-Gelsemine

Tool inhibitors and assays to interrogate the biology of the TRAF2 and NCK interacting kinase

Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition

Aza-Cope Rearrangement−Mannich Cyclizations for the Formation of Complex Tricyclic Amines: Stereocontrolled Total Synthesis of (±)-Gelsemine

High Fidelity Suzuki–Miyaura Coupling for the Synthesis of DNA Encoded Libraries Enabled by Micelle Forming Surfactants

Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}- N -methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs

Functional Group Tolerance of a Micellar on-DNA Suzuki–Miyaura Cross-Coupling Reaction for DNA-Encoded Library Design

Screening Ultra-Large Encoded Compound Libraries Leads to Novel Protein–Ligand Interactions and High Selectivity

Scope of on-DNA nucleophilic aromatic substitution on weakly-activated heterocyclic substrates for the synthesis of DNA-encoded libraries

Synthesis of Structurally Diverse N‐Substituted Quaternary‐Carbon‐Containing Small Molecules from α,α‐Disubstituted Propargyl Amino Esters

Partially Saturated Bicyclic Heteroaromatics as an sp(3) -Enriched Fragment Collection

A small-molecule PI3Kα activator for cardioprotection and neuroregeneration

Highly efficient on-DNA amide couplings promoted by micelle forming surfactants for the synthesis of DNA encoded libraries

Discovery of a selective c-MET inhibitor with a novel binding mode

AiZynth impact on medicinal chemistry practice at AstraZeneca

Abstract 296: Structure-based and property-based drug design of AZD5305, a highly selective PARP1 inhibitor and trapper

Discovery of 5‑{4-[(7-Ethyl-6-oxo‑5,6-dihydro‑1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}‑N‑methylpyridine-2-carboxamide (AZD5305): A PARP1–DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs

Discovery of Spiro-azaindoline Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1)

Partially Saturated Bicyclic Heteroaromatics as an sp 3 ‐Enriched Fragment Collection

Controlling stereoselection in intramolecular heck reactions by tailoring the palladium catalyst

Partially Saturated Bicyclic Heteroaromatics as an sp3-Enriched Fragment Collection

Identification and optimisation of a series of tetrahydrobenzotriazoles as metabotropic glutamate receptor 5-selective positive allosteric modulators that improve performance in a preclinical model of cognition

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