Frederick W Goldberg
Frederick W Goldberg
Global Project Leader (Senior Director), Oncology R&D, AstraZeneca
Verified email at
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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
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
Straightforward strategies for the preparation of NH-sulfoximines: a serendipitous story
JA Bull, L Degennaro, R Luisi
Synlett 28 (19), 2525-2538, 2017
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
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
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
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
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
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
Kinase Drug Discovery: Modern Approaches
FW Goldberg, RA Ward
Royal Society of Chemistry, 2019
A one-step synthesis of tetrahydropyranopyranones from carbonyl compounds
A Armstrong, FW Goldberg, DA Sandham
Tetrahedron Letters 42 (27), 4585-4587, 2001
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
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
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
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
Evolution of small molecule kinase drugs
HL Lightfoot, FW Goldberg, J Sedelmeier
ACS Medicinal Chemistry Letters 10 (2), 153-160, 2018
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
Synthesis of Functionalized Pyrazolo [1, 5-a] pyridines:[3+ 2] Cycloaddition of N-Aminopyridines and α, β-Unsaturated Carbonyl Compounds/Alkenes at Room Temperature
C Ravi, S Samanta, DC Mohan, NNK Reddy, S Adimurthy
Synthesis 49 (11), 2513-2522, 2017
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
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
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