| AZD7648 is a potent and selective DNA-PK inhibitor that enhances radiation, chemotherapy and olaparib activity JHL Fok, A Ramos-Montoya, M Vazquez-Chantada, PWG Wijnhoven, ... Nature communications 10 (1), 5065, 2019 | 207 | 2019 |
| Designing novel building blocks is an overlooked strategy to improve compound quality FW Goldberg, JG Kettle, T Kogej, MWD Perry, NP Tomkinson Drug Discovery Today 20 (1), 11-17, 2015 | 188 | 2015 |
| Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) JS Scott, FW Goldberg, AV Turnbull Journal of Medicinal Chemistry 57 (11), 4466-4486, 2014 | 97 | 2014 |
| An Expedient Formal Total Synthesis of (−)-Diazonamide A via a Powerful, Stereoselective O-Aryl to C-Aryl Migration To Form the C10 Quaternary Center CM Cheung, FW Goldberg, P Magnus, CJ Russell, R Turnbull, V Lynch Journal of the American Chemical Society 129 (40), 12320-12327, 2007 | 89 | 2007 |
| General synthetic strategies towards N-alkyl sulfoximine building blocks for medicinal chemistry and the use of dimethylsulfoximine as a versatile precursor FW Goldberg, JG Kettle, J Xiong, D Lin Tetrahedron 70 (37), 6613-6622, 2014 | 75 | 2014 |
| Structure-Based Design and Pharmacokinetic Optimization of Covalent Allosteric Inhibitors of the Mutant GTPase KRASG12C JG Kettle, SK Bagal, S Bickerton, MS Bodnarchuk, J Breed, RJ Carbajo, ... Journal of medicinal chemistry 63 (9), 4468-4483, 2020 | 56 | 2020 |
| 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 … FW Goldberg, MRV Finlay, AKT Ting, D Beattie, GM Lamont, C Fallan, ... Journal of Medicinal Chemistry 63 (7), 3461-3471, 2019 | 52 | 2019 |
| Asymmetric synthesis of 2-alkyl-substituted tetrahydroquinolines by an enantioselective aza-Michael reaction LL Taylor, FW Goldberg, KKM Hii Organic & Biomolecular Chemistry 10 (22), 4424-4432, 2012 | 43 | 2012 |
| Kinase Drug Discovery: Modern Approaches FW Goldberg, RA Ward Royal Society of Chemistry, 2019 | 39* | 2019 |
| A one-step synthesis of tetrahydropyranopyranones from carbonyl compounds A Armstrong, FW Goldberg, DA Sandham Tetrahedron Letters 42 (27), 4585-4587, 2001 | 39 | 2001 |
| Rapid generation of a high quality lead for transforming growth factor-β (TGF-β) type I receptor (ALK5) FW Goldberg, RA Ward, SJ Powell, JÉ Debreczeni, RA Norman, ... Journal of medicinal chemistry 52 (23), 7901-7905, 2009 | 35 | 2009 |
| A Mild Thermal and Acid-Catalyzed Rearrangement of O-Aryl Ethers into ortho-Hydroxy Arenes FW Goldberg, P Magnus, R Turnbull Organic Letters 7 (20), 4531-4534, 2005 | 35 | 2005 |
| Free-Wilson and structural approaches to co-optimizing human and rodent isoform potency for 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors FW Goldberg, AG Leach, JS Scott, WL Snelson, SD Groombridge, ... Journal of Medicinal Chemistry 55 (23), 10652-10661, 2012 | 32 | 2012 |
| Evolution of small molecule kinase drugs HL Lightfoot, FW Goldberg, J Sedelmeier ACS Medicinal Chemistry Letters 10 (2), 153-160, 2018 | 30 | 2018 |
| Direct targeting of FOXP3 in Tregs with AZD8701, a novel antisense oligonucleotide to relieve immunosuppression in cancer A Revenko, LS Carnevalli, C Sinclair, B Johnson, A Peter, M Taylor, ... Journal for Immunotherapy of Cancer 10 (4), 2022 | 27 | 2022 |
| Design of pyrazolo-pyrimidines as 11β-HSD1 inhibitors through optimisation of molecular electrostatic potential GR Robb, S Boyd, CD Davies, AG Dossetter, FW Goldberg, PD Kemmitt, ... MedChemComm 6 (5), 926-934, 2015 | 26 | 2015 |
| Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRASG12C JG Kettle, SK Bagal, S Bickerton, MS Bodnarchuk, S Boyd, J Breed, ... Journal of Medicinal Chemistry 65 (9), 6940-6952, 2022 | 25 | 2022 |
| Optimization of brain penetrant 11β-hydroxysteroid dehydrogenase type I inhibitors and in vivo testing in diet-induced obese mice FW Goldberg, AG Dossetter, JS Scott, GR Robb, S Boyd, SD Groombridge, ... Journal of Medicinal Chemistry 57 (3), 970-986, 2014 | 25 | 2014 |
| Optimization of highly kinase selective bis-anilino pyrimidine PAK1 inhibitors W McCoull, EJ Hennessy, K Blades, C Chuaqui, JE Dowling, ... ACS Medicinal Chemistry Letters 7 (12), 1118-1123, 2016 | 24 | 2016 |
| Identification and optimisation of 7-azaindole PAK1 inhibitors with improved potency and kinase selectivity W McCoull, EJ Hennessy, K Blades, MR Box, C Chuaqui, JE Dowling, ... MedChemComm 5 (10), 1533-1539, 2014 | 24 | 2014 |
Jason Grant KettlePrincipal Scientist, Medicinal Chemistry, Oncology iMED, AstraZenecaVerified email at astrazeneca.com
