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

M. Raymond V. Finlay, Mark J. Anderton, Susan Ashton, +33

Journal of Medicinal Chemistry

GeneticsPathologyClinical CandidateTumor BiologyT790m Resistance Mutations +16

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

Jacqueline H. L. Fok, Antonio Ramos‐Montoya, Mercedes Vázquez–Chantada, +22

Nature Communications

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

Frederick W. Goldberg, M. Raymond V. Finlay, Attilla Ting, +13

Journal of Medicinal Chemistry

PharmacotherapyChemical BiologyDna-pk Catalytic SubunitPharmaceutical ChemistryPre-clinical Pharmacology +18

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

Jason G. Kettle, Sharan K. Bagal, Sue Bickerton, +39

Journal of Medicinal Chemistry

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

Frederick W. Goldberg, Jason G. Kettle, Gillian M. Lamont, +13

Journal of Medicinal Chemistry

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

Sébastien L. Degorce, Andrew Bailey, Rowena Callis, +13

Journal of Medicinal Chemistry

Breast OncologyFemale Reproductive FunctionPharmacotherapyMolecular PharmacologyMedicinal Chemistry +17

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

M. Raymond V. Finlay, David Buttar, Susan E. Critchlow, +11

Bioorganic & Medicinal Chemistry Letters

Drug TargetBiochemistryMedicineNatural SciencesRational Drug Design +7

Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors

William McCoull, Edward J. Hennessy, Kevin Blades, +11

ACS Medicinal Chemistry Letters

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

Jason G. Kettle, Sharan K. Bagal, Derek Barratt, +42

Journal of Medicinal Chemistry

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

Paul A. Bethel, Andrew D. Campbell, Frederick W. Goldberg, +3

Tetrahedron

Cross-coupling ReactionEngineeringHeterocyclicOrganic ChemistryChemistry +2