P. Kemmitt

发表

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.

Peter Ballard, Simon J Brown, Nathaniel G. Martin, 2014, 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.

Tumour regression and improved gastrointestinal tolerability from controlled release of SN‐38 from novel polyoxazoline‐modified dendrimers

Jennifer I. Hare, M. Waring, S. Barry, 2017, Journal of controlled release : official journal of the Controlled Release Society.

Enhanced cytocompatibility and functional group content of poly(L-lysine) dendrimers by grafting with poly(oxazolines)

Jennifer I. Hare, M. Waring, S. Barry, 2016 .

Development of a novel BCL6 PROTAC to provide insight into small molecule targeting of BCL6

David M. Wilson, Qing Cao, M. Waring, 2018 .

Development of a Novel B-Cell Lymphoma 6 (BCL6) PROTAC To Provide Insight into Small Molecule Targeting of BCL6.

David M. Wilson, Qing Cao, M. Waring, 2018, ACS chemical biology.

Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors.

Matthew Grist, C. Chuaqui, Qing Cao, 2017, Journal of medicinal chemistry.

Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).

Magnus J. Johansson, Tobias Noeske, Robert D. M. Davies, 2012, Journal of medicinal chemistry.

Deliberately Losing Control of C−H Activation Processes in the Design of Small‐Molecule‐Fragment Arrays Targeting Peroxisomal Metabolism

J. Spencer, P. Brennan, F. Delft, 2020, ChemMedChem.

Design and optimisation of dendrimer-conjugated Bcl-2/xL inhibitor, AZD0466, with improved therapeutic index for cancer therapy

E. Hennessy, S. Fawell, B. Davies, 2021, Communications biology.

Discovery of a potent, selective, and orally efficacious pyrimidinooxazinyl bicyclooctaneacetic acid diacylglycerol acyltransferase-1 inhibitor.

A. Turnbull, P. Kemmitt, A. Birch, 2009, Journal of medicinal chemistry.

Identification of a novel series of azabenzimidazole-derived inhibitors of spleen tyrosine kinase.

Peng-Fei Wang, J. Patel, B. Barlaam, 2020, Bioorganic & medicinal chemistry letters.

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

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

Combining Sanford Arylations on Benzodiazepines with the Nuisance Effect

J. Atack, S. Coles, G. Tizzard, 2017, Advanced synthesis & catalysis.

Gram-Scale Laboratory Synthesis of TC AC 28, a High-Affinity BET Bromodomain Ligand

J. Spencer, A. Ciulli, M. Baud, 2017, ACS omega.

1—Azatriene cyclisation as a route to annelated pyrido[4,3-b]indoles

P. Kemmitt, T. L. Gilchrist, A. L. Germain, 1997 .

Electrocyclic Ring Closure of 1-Azatrienes as a Route to the Indolo[3,2,1-ij][1,6]naphthyridine Ring System

P. Kemmitt, T. L. Gilchrist, A. L. Germain, 1994 .

Regioselective routes to orthogonally-substituted aromatic MIDA boronates.

J. Spencer, P. Kemmitt, S. Mark Roe, 2016, Organic & biomolecular chemistry.

Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.

Andrew G. Leach, A. Plowright, Robert D. M. Davies, 2012, Bioorganic & medicinal chemistry letters.

Microwave-mediated synthesis of N-methyliminodiacetic acid (MIDA) boronates

J. Spencer, P. Kemmitt, Adam J. Close, 2014 .

Synthesis of 3-(hetero)aryl tetrahydropyrazolo[3,4-c]pyridines by Suzuki-Miyaura cross-coupling methodology.

G. Lamont, Matthew R. Box, P. Kemmitt, 2014, The Journal of organic chemistry.

Oxidative radical cyclisations for the synthesis of gamma-lactones.

D. G. Hulcoop, P. Kemmitt, J. Burton, 2008, Chemical communications.

N 1-Arylation of 1,4-Benzodiazepine-2-ones with Diaryliodonium Salts

S. Coles, G. Tizzard, J. Spencer, 2017, Synlett.

Late stage C―H activation of a privileged scaffold; synthesis of a library of benzodiazepines

S. Coles, G. Tizzard, J. Spencer, 2016 .

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.

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 .

Elaboration of tetra-orthogonally-substituted aromatic scaffolds towards novel EGFR-kinase inhibitors.

Rhiannon N. Jones, S. Roe, J. Spencer, 2016, Organic & biomolecular 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.

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

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

Making medicinal chemistry more effective--application of Lean Sigma to improve processes, speed and quality.

Nidhal Selmi, Jan Kihlberg, Magnus J. Johansson, 2009, Drug discovery today.

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

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

Atom and step economical synthesis of acyclic quaternary centers via iridium-catalyzed hydroarylative cross-coupling of 1,1-disubstituted alkenes

Matthew N. Grayson, Lyman J. L. Feron, P. Kemmitt, 2022, Chemical science.

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.

Optimisation of biphenyl acetic acid inhibitors of diacylglycerol acetyl transferase 1 – the discovery of AZD2353

Andrew G. Leach, M. Waring, P. Macfaul, 2013 .

Design and synthesis of a novel series of cyclohexyloxy-pyridyl derivatives as inhibitors of diacylglycerol acyl transferase 1

Andrew G. Leach, A. Plowright, M. Waring, 2013 .

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.

Design and optimisation of dendrimer-conjugated Bcl-2/xL inhibitor, AZD0466, with improved therapeutic index for cancer therapy

E. Hennessy, S. Fawell, B. Davies, 2021, Communications Biology.

Magnus J. Johansson, Tobias Noeske, Robert D. M. Davies, 2012, Journal of medicinal chemistry.