Frederick W. Goldberg

发表

General synthetic strategies towards N-alkyl sulfoximine building blocks for medicinal chemistry and the use of dimethylsulfoximine as a versatile precursor

Jason G. Kettle, J. Kettle, Frederick W. Goldberg, 2014 .

Selective Kinase Inhibitors in Cancer

A. Mortlock, D. Wilson, J. Kettle, 2017 .

Evolution of Small Molecule Kinase Drugs.

J. Sedelmeier, H. Lightfoot, Frederick W. Goldberg, 2018, ACS medicinal chemistry letters.

Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1).

James S. Scott, A. Turnbull, Frederick W. Goldberg, 2014, Journal of medicinal chemistry.

Free-Wilson and structural approaches to co-optimizing human and rodent isoform potency for 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors.

Andrew G. Leach, James S. Scott, Frederick W. Goldberg, 2012, Journal of medicinal chemistry.

Designing novel building blocks is an overlooked strategy to improve compound quality.

Matthew W D Perry, Thierry Kogej, Frederick W Goldberg, 2015, Drug discovery today.

Design of pyrazolo-pyrimidines as 11β-HSD1 inhibitors through optimisation of molecular electrostatic potential

James S. Scott, G. Robb, J. Swales, 2015 .

Optimization of brain penetrant 11β-hydroxysteroid dehydrogenase type I inhibitors and in vivo testing in diet-induced obese mice.

James S. Scott, A. Turnbull, T. Sjögren, 2014, Journal of medicinal chemistry.

11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitors Still Improve Metabolic Phenotype in Male 11β-HSD1 Knockout Mice Suggesting Off-Target Mechanisms

M. Bohlooly-y, A. Turnbull, Anne White, 2013, Endocrinology.

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.

B. Davies, M. Vázquez‐Chantada, G. Lamont, 2019, Journal of medicinal chemistry.

Optimization of a Series of Potent, Selective and Orally Bioavailable SYK Inhibitors.

David M. Wilson, Peng-Fei Wang, S. Fawell, 2009, Bioorganic & medicinal chemistry letters.

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

M. O’Connor, S. Fawell, B. Davies, 2019, Nature Communications.

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

G. Lamont, Paul A. Bethel, P. Kemmitt, 2012 .

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

G. Lamont, D. Buttar, S. Critchlow, 2022, Journal of medicinal chemistry.

Structure-based design and pharmacokinetic optimization of covalent allosteric inhibitors of the mutant GTPase KRASG12C.

Doyle J Cassar, J. Breed, D. Ogg, 2020, Journal of medicinal chemistry.

Direct targeting of FOXP3 in Tregs with AZD8701, a novel antisense oligonucleotide to relieve immunosuppression in cancer

S. Barry, G. Kar, P. Lyne, 2022, Journal for ImmunoTherapy of Cancer.

Chemical Biology Approaches Confirm MCT4 as the Therapeutic Target of a Cellular Optimized Hit.

G. Lamont, M. P. Castaldi, Andrew X. Zhang, 2023, ACS chemical biology.

Discovery of AZD4747, a Potent and Selective Inhibitor of Mutant GTPase KRASG12C with Demonstrable CNS Penetration.

Doyle J Cassar, Nichola L. Davies, J. Breed, 2023, Journal of medicinal chemistry.