F. Goldberg

发表

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.

Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors.

E. Hennessy, C. Chuaqui, A. Ferguson, 2016, ACS medicinal chemistry letters.

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.

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 .

Asymmetric synthesis of 2-alkyl-substituted tetrahydroquinolines by an enantioselective aza-Michael reaction.

K. K. Hii, F. Goldberg, Laura L. Taylor, 2012, Organic & biomolecular chemistry.

An expedient formal total synthesis of (-)-diazonamide A via a powerful, stereoselective O-aryl to C-aryl migration to form the C10 quaternary center.

V. Lynch, P. Magnus, Rachel Turnbull, 2007, Journal of the American Chemical Society.

A mild thermal and acid-catalyzed rearrangement of O-aryl ethers into ortho-hydroxy arenes.

P. Magnus, Rachel Turnbull, F. Goldberg, 2005, Organic letters.

Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRASG12C.

Doyle J Cassar, Nichola L. Davies, J. Breed, 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.

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 .

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

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

Selective Kinase Inhibitors in Cancer

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

Preclinical Evaluation of AZ12601011 and AZ12799734, Inhibitors of Transforming Growth Factor β Superfamily Type 1 Receptors

S. Barry, O. Sansom, G. Inman, 2018, Molecular Pharmacology.

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.

Kinase Drug Discovery

R. Ward, F. Goldberg, 2011 .

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.

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.

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.

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

Cristian Bodin, Andrew G Leach, James S. Scott, 2012, Journal of medicinal chemistry.

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.

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.

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

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

Evolution of Small Molecule Kinase Drugs.

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

Identification and optimisation of 7-azaindole PAK1 inhibitors with improved potency and kinase selectivity

E. Hennessy, C. Chuaqui, A. Ferguson, 2014 .

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.

The changing landscape of cancer drug discovery: a challenge to the medicinal chemist of tomorrow.

A. C. Rigby, S. Snyder, C. Leamon, 2009, Drug discovery today.

Discovery and optimization of efficacious neutral 4-amino-6-biphenyl-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5-one diacylglycerol acyl transferase-1 (DGAT1) inhibitors

A. Leach, Wendy L. Snelson, A. Birch, 2013 .

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

B. Davies, M. Vázquez‐Chantada, G. Lamont, 2022, ACS medicinal chemistry letters.

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.

Abstract 1207: Reversing lactate-driven immunosuppression using the novel, potent and selective MCT4 inhibitor AZD0095

S. Critchlow, G. Hughes, E. Hardaker, 2019, Experimental and Molecular Therapeutics.