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Antitumor Activity of Osimertinib, an Irreversible Mutant-Selective EGFR Tyrosine Kinase Inhibitor, in NSCLC Harboring EGFR Exon 20 Insertions

Molecular cancer therapeutics, 2018-05, Vol.17 (5), p.885-896

2018

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Selective DNA-PKcs inhibition extends the therapeutic index of localized radiotherapy and chemotherapy

The Journal of clinical investigation, 2020-01, Vol.130 (1), p.258-271

2020

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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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Discovery of a Potent and Selective EGFR Inhibitor (AZD9291) of Both Sensitizing and T790M Resistance Mutations That Spares the Wild Type Form of the Receptor

Journal of medicinal chemistry, 2014-10, Vol.57 (20), p.8249-8267

2014

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Small Molecule Binding Sites on the Ras:SOS Complex Can Be Exploited for Inhibition of Ras Activation

Journal of medicinal chemistry, 2015-03, Vol.58 (5), p.2265-2274

2015

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Potent and Selective Inhibitors of the Epidermal Growth Factor Receptor to Overcome C797S-Mediated Resistance

Journal of medicinal chemistry, 2021-09, Vol.64 (18), p.13704-13718

2021

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Modulation of DNA repair by pharmacological inhibitors of the PIKK protein kinase family

Bioorganic & medicinal chemistry letters, 2012-09, Vol.22 (17), p.5352-5359

2012

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DNA-dependent protein kinase (DNA-PK) inhibitors: Structure–activity relationships for O-alkoxyphenylchromen-4-one probes of the ATP-binding domain

Bioorganic & medicinal chemistry letters, 2011-02, Vol.21 (3), p.966-970

2011

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Discovery of AZD3147: A Potent, Selective Dual Inhibitor of mTORC1 and mTORC2

Journal of medicinal chemistry, 2015-03, Vol.58 (5), p.2326-2349

2015

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AZD7648 is a potent and selective DNA-PK inhibitor that enhances radiation, chemotherapy and olaparib activity

Nature communications, 2019-11, Vol.10 (1), p.5065-15, Article 5065

2019

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Sulfonyl-morpholino-pyrimidines: SAR and development of a novel class of selective mTOR kinase inhibitor

Bioorganic & medicinal chemistry letters, 2012-06, Vol.22 (12), p.4163-4168

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

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

2020

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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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Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors

Bioorganic & medicinal chemistry, 2008-12, Vol.18 (24), p.6486-6489

2008

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Imidazole piperazines: SAR and development of a potent class of cyclin-dependent kinase inhibitors with a novel binding mode

Bioorganic & medicinal chemistry, 2008-08, Vol.18 (15), p.4442-4446

2008

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Novel Arginase Inhibitor, AZD0011, Demonstrates Immune Cell Stimulation and Antitumor Efficacy with Diverse Combination Partners

Molecular cancer therapeutics, 2023-05, Vol.22 (5), p.630-645

2023

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Correction to “Discovery of a Thiadiazole–Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models”

Journal of medicinal chemistry, 2023-07, Vol.66 (13), p.9223-9224

2023

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Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors

Bioorganic & medicinal chemistry, 2008-10, Vol.18 (20), p.5487-5492

2008

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The structure-guided discovery of osimertinib: the first U.S. FDA approved mutant selective inhibitor of EGFR T790M

MedChemComm, 2017-05, Vol.8 (5), p.820-822

2017

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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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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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Potential strategies for increasing drug-discovery productivity

Future medicinal chemistry, 2014-04, Vol.6 (5), p.515

2014

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Antitumor Activity of Osimertinib, an Irreversible Mutant-Selective EGFR Tyrosine Kinase Inhibitor, in NSCLC Harboring EGFR Exon 20 Insertions

Selective DNA-PKcs inhibition extends the therapeutic index of localized radiotherapy and chemotherapy

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

Discovery of a Potent and Selective EGFR Inhibitor (AZD9291) of Both Sensitizing and T790M Resistance Mutations That Spares the Wild Type Form of the Receptor

AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer

Small Molecule Binding Sites on the Ras:SOS Complex Can Be Exploited for Inhibition of Ras Activation

Potent and Selective Inhibitors of the Epidermal Growth Factor Receptor to Overcome C797S-Mediated Resistance

Discovery of a Thiadiazole–Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models

Modulation of DNA repair by pharmacological inhibitors of the PIKK protein kinase family

DNA-dependent protein kinase (DNA-PK) inhibitors: Structure–activity relationships for O-alkoxyphenylchromen-4-one probes of the ATP-binding domain

Discovery of AZD3147: A Potent, Selective Dual Inhibitor of mTORC1 and mTORC2

Preclinical Comparison of the Blood-brain barrier Permeability of Osimertinib with Other EGFR TKIs

AZD7648 is a potent and selective DNA-PK inhibitor that enhances radiation, chemotherapy and olaparib activity

Sulfonyl-morpholino-pyrimidines: SAR and development of a novel class of selective mTOR kinase inhibitor

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

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

Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors

Imidazole piperazines: SAR and development of a potent class of cyclin-dependent kinase inhibitors with a novel binding mode

Novel Arginase Inhibitor, AZD0011, Demonstrates Immune Cell Stimulation and Antitumor Efficacy with Diverse Combination Partners

Correction to “Discovery of a Thiadiazole–Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models”

Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors

The structure-guided discovery of osimertinib: the first U.S. FDA approved mutant selective inhibitor of EGFR T790M

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

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

Potential strategies for increasing drug-discovery productivity

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