Publications

A second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral bioavailability. Charrier, Nicolas; Clarke, Brian; Cutler, Leanne; Demont, Emmanuel; Dingwall, Colin; Dunsdon, Rachel; East, Philip; Hawkins, Julie; Howes, Colin; Hussain, Ishrut; Jeffrey, Philip; Maile Graham, Matico Rosalie, Mosley Julie, Naylor Alan, O’Brien Alistair, Redshaw Sally, Rowland, Paul; Soleil, Virginie; Smith, Kathrine J; Sweitzer, Sharon; Theobald, Pam; Vesey, David; Walter, Daryl S; Wayne, Gareth. J. Med. Chem., 2008, 51 (11), 3313-3317.

BACE-1 inhibitors part 3: Identification of hydroxyl ethylamines (HEAs) with nanomolar potency in cells. Beswick, Paul; Charrier, Nicolas; Clarke, Brian; Demont, Emmanuel; Dingwall, Colin; Dunsdon, Rachel; Faller, Andrew; Gleave, Robert; Hawkins, Julie; Hussain, Ishrut; Johnson, Christopher; MacPherson, David; Maile, Graham; Matico, Rosalie; Milner, Peter; Mosley, Julie; Naylor, Alan; O’Brien, Alistair; Redshaw, Sally; Riddell, David; Rowland, Paul; Skidmore, John; Soleil, Virginie; Smith, Kate; Stanway, Steven; Stemp, Geoff; Stuart, Alistair; Sweitzer, Sharon; Theobald, Pam; Vesey, David; Walter, Daryl S; Ward, John; Wayne, Gareth. Bioorganic & Medicinal Chemistry Letters, 2008, 18(3), 1022-1026.

BACE-1 inhibitors part 2: Identification of hydroxyl ethylamines (HEAs) with reduced peptidic character. Clarke, Brian; Demont, Emmanuel; Dingwall, Colin; Dunsdon, Rachel; Faller, Andrew; Hawkins, Julie; Hussain, Ishrut; MacPherson, David; Maile, Graham; Matico, Rosalie; Milner, Peter; Mosley, Julie; Naylor, Alan; O’Brien, Alistair; Redshaw, Sally; Riddell, David; Rowland, Paul; Soleil, Virginie; Smith, Kate; Stanway, Steven; Stemp, Geoff; Sweitzer, Sharon; Theobald, Pam; Vesey, David; Walter, Daryl S; Ward, John; Wayne, Gareth. Bioorganic & Medicinal Chemistry Letters, 2008, 18(3), 1017-1021.

BACE-1 inhibitors part 1: Identification of novel hydroxyl ethylamines (HEAs). Clarke, Brian; Demont, Emmanuel; Dingwall, Colin; Dunsdon, Rachel; Faller, Andrew; Hawkins, Julie; Hussain, Ishrut; MacPherson, David; Maile, Graham; Matico, Rosalie; Milner, Peter; Mosley, Julie; Naylor, Alan; O’Brien, Alistair; Redshaw, Sally; Riddell, David; Rowland, Paul; Soleil, Virginie; Smith, Kate; Stanway, Steven; Stemp, Geoff; Sweitzer, Sharon; Theobald, Pam; Vesey, David; Walter, Daryl S; Ward, John; Wayne, Gareth. Bioorganic & Medicinal Chemistry Letters, 2008, 18(3), 1011-1016.

Oral administration of a potent and selective non-peptidic BACE-1 inhibitor decreases β-cleavage of amyloid precursor protein and amyloid-β production in vivo. Hussain, Ishrut; Hawkins, Julie; Harrison, David; Hille, Christopher; Wayne, Gareth; Cutler, Leanne; Buck, Tania; Walter, Daryl; Demont, Emmanuel; Howes, Colin; Naylor, Alan; Jeffrey, Philip; Gonzalez, Maria I.; Dingwall, Colin; Michel, Anton; Redshaw, Sally; Davis, John B. Journal of Neurochemistry, 2007, 100(3), 802-809.

Synthesis of indoles: efficient functionalization of the 7-position. Charrier, Nicolas; Demont, Emmanuel; Dunsdon, Rachel; Maile, Graham; Naylor, Alan; O’Brien, Alistair; Redshaw, Sally; Theobald, Pam; Vesey, David; Walter, Daryl. Synthesis, 2006, 20, 3467-3477.

SkelGen: a general tool for structure-based de novo ligand design. Philip M Dean, Stuart Firth-Clark, William Harris, Stewart B Kirton, Nikolay P Todorov. Expert Opinion on Drug Discovery, 2006, 1(2), 179-189.

Generation and Selection of Novel Estrogen Receptor Ligands Using the De Novo Structure-Based Design Tool, SkelGen. Firth-Clark, S., Willems, H.M.G., Williams, A. and Harris, W. Journal of Chemical Information and Modelling, 46 (2), 642 -647, 2006.

Synthesis of 3,5,7-substituted indoles via Heck cyclization. Charrier, Nicolas; Demont, Emmanuel; Dunsdon, Rachel; Maile, Graham; Naylor, Alan; O’Brien, Alistair; Redshaw, Sally; Theobald, Pam; Vesey, David; Walter, Daryl. Synlett, 2005, 20, 3071-3074.

HIV protease inhibitors. Part 2: [3+2] cycloaddition, isomerization; and ring expansion en route to 4,5-substituted cyclohexenones. Demont, Emmanuel; Eatherton, Andrew; Frampton, Christopher S.; Kahn, Irfan; Redshaw, Sally. Synlett, 2004, 4, 684-687.

HIV protease inhibitors. Part 1: Use of Evans’ oxazolidinone in intermolecular Diels-Alder reaction en route to 3,4-substituted cyclohexanones. Crackett, Peter; Demont, Emmanuel; Eatherton, Andrew; Frampton, Christopher S.; Gilbert, Jenny; Kahn, Irfan; Redshaw, Sally; Watson, William. Synlett, 2004, 4, 679-683.

Development of a Virtual Screening Method for Identification of “Frequent Hitters” in Compound Libraries. Roche, O.; Schneider, P.; Zuegge, J.; Guba, W.; Kansy, M.; Alanine, A.; Bleicher, K.; Danel, F.; Gutknecht, E.-M.; Rogers-Evans, M.; Neidhart, W.; Stalder, H.; Dillon, M.; Sjogren, E.; Fotouhi, N.; Gillespie, P.; Goodnow, R.; Harris, W.; Jones, P.; Taniguchi, M.; Tsujii, S.; von der Saal, W.; Zimmermann, G.; Schneider, G.; J. Med. Chem.; 2002; 45(1); 137-142.

Structure-based design of peptidomimetic antagonists of p56lck SH2 domain. Christopher J. Hobbs, Rino A. Bit, Andrew D. Cansfield, Bill Harris, Christopher H. Hill, Katherine L. Hilyard, Ian R. Kilford, Eric Kitas, Antonin Kroehn, Peter Lovell, David Pole, Paul Rugman, Brad S. Sherborne, Ian E. D. Smith, David R. Vesey, D. Lee Walmsley, David Whittaker, Glyn Williams, Fiona Wilson, David Banner, Allan Surgenor and Neera Borkakoti. Bioorganic and Medicinal Chemistry Letters, 2002, 12(10), 1365-1369.

Catalytic Electronic Activation: Indirect Addition of Nucleophiles to an Allylic Alcohol. Phillip J. Black, William Harris and Jonathan M. J. Williams. Angew. Chem. Int. Ed., 2001, 40(23), 4475-4476.

Fusion and Entry Inhibitors as Therapies for HIV. Redshaw S, Westby M. Expert Opinion on Emerging Drugs, 2001, 6(2), 209-224.

Discovery and Early Development of Saquinavir. Duncan IB, Redshaw S. in Protease Inhibitors in AIDS Therapy eds. Ogden RC, Flexner CW; Marcel Dekker Inc., New York, 2001, 27-47.

Selective tyrosine kinase inhibitors. Wilkinson, Sandra E.; Harris, William. Emerging Drugs, 2000, 5(3), 287-297.

Stereoselectivity, regioselectivity and mechanism in the intramolecular ‘citran’ bicyclization of chromenes. Calderon-Higginson C, Crombie L, Redshaw S, Whiting DA. J. Chem. Soc. Perkin Trans. 1, 2000, 15, 2491-2494.

The road to Fortovase. A history of saquinavir, the first human immunodeficiency virus protease inhibitor. Redshaw S, Roberts NA, Thomas GJ. Handb. Exp. Pharmacol., 2000, 140 (Proteases as Targets for Therapy), 3-21.

Inhibitors of HIV Protease. Redshaw S, Thomas GJ. in Antivirals Against AIDS. eds. Unger RE, Kreuter J, Rubsamen-Waigmann H; Marcel Dekker Inc., New York, 2000, 151-180.

The bisindolylmaleimide protein kinase C inhibitor, Ro 32-2241, reverses multidrug resistance in KB tumor cells. Merritt, Janet E.; Sullivan, John A.; Drew, Lisa; Khan, Abida; Wilson, Kevin; Mulqueen, Michael; Harris, William; Bradshaw, David; Hill, Christopher H.; Rumsby, Martin; Warr, Roger Cancer Chemother. Pharmacol., 1999, 43(5), 371-378.

Selective racemization of esters: relevance to enzymic hydrolysis reactions. Dinh, Phi M.; Williams, Jonathan M. J.; Harris, William. Tetrahedron Lett., 1999, 40(4), 749-752.

Dynamic kinetic resolution using enzymes and transition metals combination. Dinh, P. M.; El Gihani, M. T.; Williams, J. M. J.; Harris, W. Chim. Oggi, 1998, 16(7/8), 42-44.

The design of a selective inhibitor of HIV proteinase. Redshaw S. Protein Eng., 1997, 10 (Suppl.), 77.

Human immunodeficiency virus protease inhibitors. Redshaw S, Thomas GJ. Emerging Drugs, 1997, 2, 127-154.

Recent developments in protein kinase C inhibitors. Harris, W.; Wilkinson, S. E.; Nixon, J. S. Expert Opin. Ther. Pat., 1997, 7(1), 63-68.

Catalytic racemization of alcohols: applications to enzymic resolution reactions. Dinh, Phi M.; Howarth, Judith A.; Hudnott, Anna R.; Williams, Jonathan M. J.; Harris, William. Tetrahedron Lett., 1996, 37(42), 7623-7626.

Inhibitors of HIV Proteinase. Kinchington D, Redshaw S. in Antiviral Chemotherapy eds. Jeffries DJ, de Clercq E, Wiley, Chichester, 1995, 3-40.

Inhibitors of HIV proteinase. Martin JA, Redshaw S, Thomas GJ. Prog. Med. Chem, 1995, 32, 239-87.

Bisindolylmaleimide inhibitors of protein kinase C. Further conformational restriction of a tertiary amine side chain. Davis, Peter D.; Hallam, Trevor J.; Harris, William; Hill, Christopher H.; Lawton, Geoffrey; Nixon, John S.; Smith, Janet L.; Vesey, David R.; Wilkinson, Sandra E. Bioorg. Med. Chem. Lett., 1994, 4(11), 1303-8.

Inhibitors of HIV proteinase. Redshaw S. Expert Opin. Invest. Drugs, 1994, 3(3), 273-86.

Ro 32-0432, a selective and orally active inhibitor of protein kinase C prevents T-cell activation. Birchall A M; Bishop J; Bradshaw D; Cline A; Coffey J; Elliott L H; Gibson V M; Greenham A; Hallam T J; Harris W; Journal of Pharmacology and Experimental Therapeutics, 1994, 268(2), 922-9.

Studies toward the large-scale synthesis of the HIV proteinase inhibitor Ro 31-8959. Parkes KEB, Bushnell DJ, Crackett PH, Dunsdon SJ, Freeman AC, Gunn MP, Hopkins RA, Lambert RW, Martin JA, Merrett JH, Redshaw S, Spurden WC, Thomas GJ. J. Org. Chem., 1994, 59(13), 3656-3664.

Oxidative cyclizations with palladium acetate. A short synthesis of staurosporine aglycon. Harris, William; Hill, Christopher H.; Keech, Elizabeth; Malsher, Patrick. Tetrahedron Lett., 1993, 34(51), 8361-4.

A convenient synthesis of bisindolylmaleimides. Bit, Rino A.; Crackett, Peter H.; Harris, William; Hill, Christopher H. Tetrahedron Lett., 1993, 34(35), 5623-6.

Inhibitors of protein kinase C. 3. Potent and highly selective bisindolylmaleimides by conformational restriction. Bit, Rino A.; Davis, Peter D.; Elliott, Lucy H.; Harris, William; Hill, Christopher H.; Keech, Elizabeth; Kumar, Hari; Lawton, Geoffrey; Maw, Anna; et al. J. Med. Chem., 1993, 36(1), 21-9.

Protein Kinase C Inhibitors. Harris W., Hill C.H., Lewis E.J., Nixon J.S., Wilkinson S.E. Drugs of the Future 1993, 18(8), 727-735.

A Short Synthesis of Staurosporine Aglycone. William Harris, Christopher H. Hill, Elizabeth Keech and Patrick Malsher. Tetrahedron Lett., 1993, 34, 8361.

NMR studies of four isomers of decahydroisoquinoline-3 (S)-carboxylic acid and a potent HIV proteinase inhibitor incorporating the (S, S, S) isomer. Gilbert JC, Redshaw S, Simmonite HS, Thomas WA, Whitcombe IWA. J. Chem. Soc. Perkin Trans. 2, 1993, 3, 475-9.

Discovery and Development of the HIV Proteinase Inhibitor Ro 31-8959. Redshaw S, Roberts NA. in The Search for Antiviral Drugs: Case Histories from Concept to Clinic eds. Adams J, Meluzzi VJ. Birkhauser, Boston, 1993, 129-151.

Angiotensin-Converting Enzyme (ACE) Inhibitors and the Design of Cilazapril Redshaw S. in Medicinal Chemistry: The Role of Organic Chemistry in Drug Research eds. Ganellin CR, Roberts SM; Academic Press, London, 1993, 163-185.

Inhibitors of protein kinase C. 2. Substituted bisindolylmaleimides with improved potency and selectivity. Davis, Peter D.; Elliott, Lucy H.; Harris, William; Hill, Christopher H.; Hurst, Steven A.; Keech, Elizabeth; Kumar, M. K. Hari; Lawton, Geoffrey; Nixon, John S.; Wilkinson, Sandra E. J. Med. Chem., 1992, 35(6), 994-1001.

Novel binding mode of highly potent HIV-proteinase inhibitors incorporating the (R)-hydroxyethylamine isostere. Krohn A, Redshaw S, Ritchie JC, Graves BJ, Hatada MH. J. Med. Chem., 1991, 34(11), 3340-2.

The inhibitory activity of a peptide derivative against the growth of simian immunodeficiency virus in C8166 cells. Martin JA, Mobberley MA, Redshaw S, Burke A, Tyms AS, Ryder TA. Biochem.Biophys. Res. Commun., 1991, 176(1), 180-8.

The design of a novel class of potassium channel activating drugs, 2-(2,2-dimethylbenzopyran-4-yl)-pyridine-1-oxides. Attwood MR, Jones PS, Kay PB, Paciorek PM, Redshaw S. Life Sci., 1991, 48(8), 803-10.

Rational design of peptide-based HIV proteinase inhibitors. Roberts, Noel A.; Martin, Joseph A.; Kinchington, Derek; Broadhurst, Anne V.; Craig, J. Charles; Duncan, Ian B.; Galpin, Sarah A.; Handa, Balraj K.; Kay, John; Redshaw, Sally; et. al. Science (Washington, DC, United States), 1990, 248(4953), 358-61.

Effect of two novel inhibitors of the human immunodeficiency virus protease on the maturation of the HIV gag and gag-pol polyproteins. Overton, HA, McMillan DJ, Gridley SJ, Brenner J, Redshaw S, Mills JS. Virology (1990) 179(1): 508-11.

Angiotensin-converting enzyme inhibitors – Cilazapril and other bicyclic hexahydropyridazines. Natoff IL, Redshaw S. Drugs of the Future, 1987, 12, 475-483.

The design and synthesis of the angiotensin-converting enzyme inhibitor cilazapril and related bicyclic compounds. Attwood R, Hassall CH, Krohn A, Lawton G, Redshaw S. J. Chem. Soc. Perkin Trans. 1, 1986, 6, 1011-19.

Some inhibitors of angiotensin converting enzyme. Hassall CH, Lawton G, Moody CJ, Redshaw S. 18th Pept., Proc. Eur. Pept. Symp., 1984, 477-80.

New potent inhibitors of angiotensin converting enzyme. Attwood MR, Francis RJ, Hassall CH, Kroehn A, Lawton G, Natoff IL, Nixon JS, Redshaw S, Thomas WA. FEBS Lett., 1984, 165(2), 201-6.

Synthesis of (±)-eriobrucinol and regioisomeric monoterpenoid coumarins, using intramolecular cycloadditions. Crombie L, Redshaw SD, Slack DA, Whiting DA. J. Chem. Soc. Perkin Trans.1, 1983, 7, 1411-16.

Synthesis and structure of eriobrucinol and isomeric ‘cyclol’ meroterpenes. Crombie L, Redshaw SD, Slack DA, Whiting DA. J. Chem. Soc., Chem. Commun., 1979, 14, 628-30.

The mechanism of intramolecular ‘citran’ bicyclization of chromenes: stereochemistry of a forward (H+ catalyzed) and a related reverse (thermal) process. Crombie L, Redshaw SD, Whiting DA. J. Chem. Soc. Chem. Commun., 1979, 14, 630-1.


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