P. Macfaul

发表

Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat.

Peter D Smith, A. Rabow, R. A. Norman, 2016, ACS medicinal chemistry letters.

Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators.

R. A. Norman, James S. Scott, A. Bailey, 2015, Journal of medicinal chemistry.

Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist.

A. Rabow, D. M. Andrews, G. Walker, 2015, Journal of medicinal chemistry.

Matched molecular pairs as a guide in the optimization of pharmaceutical properties; a study of aqueous solubility, plasma protein binding and oral exposure.

Andrew G. Leach, Andrew G Leach, David A Cosgrove, 2006, Journal of medicinal chemistry.

On the utility of coupling polarised light microscopy to a solubility assay in drug discovery

P. Macfaul, A. Ratcliffe, M. Támara, 2016 .

Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors.

Alexander G. Dossetter, S. Steinbacher, P. Macfaul, 2012, Journal of medicinal chemistry.

Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition.

Alexander G. Dossetter, S. Steinbacher, P. Macfaul, 2012, Bioorganic & medicinal chemistry letters.

(1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): a potent and highly selective cathepsin K inhibitor for the treatment of osteoarthritis.

Alexander G. Dossetter, S. Steinbacher, P. Macfaul, 2012, Journal of medicinal chemistry.

Aortic Binding of AZD5248: Mechanistic Insight and Reactivity Assays To Support Lead Optimzation.

P. Macfaul, J. Tugwood, S. Swallow, 2015, Chemical research in toxicology.

Species differences in drug plasma protein binding

P. Macfaul, N. Colclough, Linette Ruston, 2014 .

Novel inhibitors of the alphavbeta3 integrin--lead identification strategy.

P. Macfaul, P. Newham, A. Morley, 2009, Bioorganic & medicinal chemistry letters.

Discovery of a series of 2-(pyridinyl)pyrimidines as potent antagonists of GPR40

M. Waring, P. Macfaul, D. Baker, 2015 .

Circumventing seizure activity in a series of G protein coupled receptor 119 (GPR119) agonists.

Hayley S. Brown, D. Laber, James S. Scott, 2014, Journal of medicinal chemistry.

Oxygen activation by metal complexes and alkyl hydroperoxides. Applications of mechanistic probes to explore the role of alkoxyl radicals in alkane functionalization

I. Arends, P. Macfaul, K. Ingold, 1997 .

Running title : Pharmacology of SERD inhibitor in breast cancer models

Graham, A. Rabow, R. A. Norman, 2016 .

Conformational restriction in a series of GPR119 agonists: differences in pharmacology between mouse and human.

Hayley S. Brown, D. Laber, James S. Scott, 2013, Bioorganic & medicinal chemistry letters.

Kinetic Solvent Effects on Hydrogen Atom Abstraction from Phenol, Aniline, and Diphenylamine. The Importance of Hydrogen Bonding on Their Radical-Trapping (Antioxidant) Activities1

P. Macfaul, K. Ingold, J. Lusztyk, 1996 .

The Titanium(IV)‐Catalyzed Epoxidation of Alkenes by tert‐Alkyl Hydroperoxides

P. Macfaul, T. Maschmeyer, John Meurig Thomas, 1996 .

Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors.

B. Barlaam, P. Macfaul, S. Pearson, 2018, ACS medicinal chemistry letters.

Use of small-molecule crystal structures to address solubility in a novel series of G protein coupled receptor 119 agonists: optimization of a lead and in vivo evaluation.

Andrew G. Leach, Hayley S. Brown, D. Laber, 2012, Journal of medicinal chemistry.

The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2 H-pyran-4-yl)-1,3-dihydro-2 H-imidazo[4,5- c]quinolin-2-one).

Nichola L. Davies, B. Barlaam, S. Degorce, 2018, Journal of medicinal chemistry.

THE ROLE OF ALKOXYL RADICALS IN GIF (GOAGGV) CHEMISTRY

P. Macfaul, D. Wayner, D. Snelgrove, 1996 .

A Radical Account of “Oxygenated Fenton Chemistry” 1

P. Macfaul, K. Ingold, A. Wayner, 1998 .

Reactions of carboxyl radicals generated by the photocleavage of complexes of iron(III) tetra(2-N-methylpyridyl)porphyrin with unsaturated and aromatic carboxylic acids in aqueous solution

P. Macfaul, B. C. Gilbert, J. Smith, 1996 .

The photoreactions of the carboxylate complexes of 5,10,15,20-tetra(2-N-methylpyridyl)porphyrin

P. Macfaul, B. C. Gilbert, J. Smith, 1997 .

PHOTO-DECARBOXYLATION OF SUBSTITUTED ALKYLCARBOXYLIC ACIDS BROUGHT ABOUT BY VISIBLE LIGHT AND IRON(III) TETRA(2-N-METHYLPYRIDYL)-PORPHYRIN IN AQUEOUS SOLUTION

P. Macfaul, B. C. Gilbert, J. Smith, 1996 .

Photolytic cleavage of the iron–carboxyalkyl ligand bond in some iron(III) tetra(N-methylpyridyl)porphyrins: evidence for reversible photodecomposition and fragmentation from EPR and UV spectroscopy

P. Macfaul, B. C. Gilbert, J. Smith, 1993 .

Exploring Iron-Plus-Hydroperoxide-Based “Oxygen Activation” Systems. Or: It’s Hard to Keep a Good Radical Down!

I. Arends, P. Macfaul, K. Ingold, 1997 .

Measurement of N-H Bond Strengths in Aromatic Amines by Photoacoustic Calorimetry(1).

P. Macfaul, K. Ingold, D. Wayner, 1997, The Journal of organic chemistry.

Spectroscopic and photochemical studies of xanthene and azo dyes on surfaces:cellophane as a mimic of paper and cotton

P. Macfaul, J. Smith, J. Oakes, 2001 .

A combined spectroscopic and crystallographic approach to probing drug-human serum albumin interactions.

David Buttar, S. Steinbacher, A. Plowright, 2010, Bioorganic & medicinal chemistry.

Hydrophobic/hydrophilic effects on the titanium(IV)- catalyzed epoxidation of cyclohexene by tert-alkyl hydroperoxides: 2-methyl-1-phenyl-2-propyl hydroperoxide (MPPH) versus tert-butyl hydroperoxide (TBHP)

P. Macfaul, John Meurig Thomas, K. Ingold, 1997 .

Selective non zinc binding inhibitors of MMP13.

D. Hargreaves, P. Macfaul, Galith Karoutchi, 2011, Bioorganic & medicinal chemistry letters.

A Radical Account of “Oxygenated Fenton Chemistry”

P. Macfaul, K. Ingold, D. Wayner, 1998 .

5-Aminopyrimidin-2-ylnitriles as cathepsin K inhibitors.

Soraya S. Porres, P. Macfaul, P. Kenny, 2009, Bioorganic & medicinal chemistry letters.

A putative monooxygenase mimic which functions via well-disguised free radical chemistry

L. Que, P. Macfaul, K. Ingold, 1997 .

Identification of pyrazolo-pyrimidinones as GHS-R1a antagonists and inverse agonists for the treatment of obesity

Nathaniel G. Martin, Robert D. M. Davies, P. Macfaul, 2013 .

AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and ESR1-Mutant Breast Tumors in Preclinical Models.

A. Rabow, G. Walker, R. A. Norman, 2016, Cancer research.

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

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

Optimisation of aqueous solubility in a series of G protein coupled receptor 119 (GPR119) agonists

Andrew G. Leach, Hayley S. Brown, James S. Scott, 2013 .

A simple in vitro assay for assessing the reactivity of nitrile containing compounds.

P. Macfaul, A. Morley, J. Crawford, 2009, Bioorganic & medicinal chemistry letters.

Achieving improved permeability by hydrogen bond donor modulation in a series of MGAT2 inhibitors

Philip A. MacFaul, Graeme R. Robb, Andrew G. Leach, 2013 .

Oxadiazole isomers: all bioisosteres are not created equal

Andrew G. Leach, James S. Scott, P. Macfaul, 2012 .

Circumventing seizure activity in a series of G protein coupled receptor 119 (GPR119) agonists.

Andrew G. Leach, Hayley S. Brown, D. Laber, 2014, Journal of medicinal chemistry.