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Journal Papers

At Sygnature Discovery we pride ourselves on being innovative and forward-thinking. We invest in the most cutting-edge technologies to deliver the best science that makes a difference to our clients.

Our commitment has successfully enabled the discovery and development of dozens of drug candidates that made it through to the clinic.

Our scientists have the expertise and the enthusiasm that often translates into novel and exciting scientific discoveries. Get up to date with our scientific breakthroughs by accessing our latest scientific publications.

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Synthesis of a hexahydropyrrolo indole (HPI) compound library

Sabrina Nickel, Philipp Nickel, Marco Hellmert, Silvia Ernst, Robert Jewell, Christopher A. Pearce, Geraint Jones, Daniel Hamza, Markus Kaisera Abstract Scaffolds of natural products represent promising starting points for the development of focused compound...

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Facile access to a heterocyclic, sp3-rich chemical scaffold via a tandem condensation/intramolecular nitrone–alkene [3+2] cycloaddition strategy

M. J. Rawling,  T. E. Storr,  W. A. Bawazir,  S. J. Cully,  W. Lewis,  M. S. I. T. Makki,  I. R. Strutt,  G. Jones,  D. Hamza  and  R. A. Stockman Abstract Scaffolds of natural...

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Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma

Stuart T. Onions, Kazuhiro Ito, Catherine E. Charron, Richard J. Brown, Marie Colucci, Fritz Frickel, George Hardy, Kevin Joly, John King-Underwood, Yasuo Kizawa, Ian Knowles, P. John Murray, Andrew Novak, Anjna Rani, Garth Rapeport,...

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Expansion of chemical space for collaborative lead generation and drug discovery: the European Lead Factory Perspective

Karawajczyk A., Giordanetto F., Benningshof J., Hamza D., Kalliokoski T., Pouwer K., Morgentin R., Nelson A., Müller G., Piechot A., Tzalis D. Abstract High-throughput screening (HTS) represents a major cornerstone of drug discovery. The...

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Expedient synthesis of an atypical oxazolidinone compound library

Sarah J. Cully, Thomas E. Storr, Michael J. Rawling, Induka R. Abeysena, Daniel Hamza, Geraint Jones, Christopher A. Pearce, Abdul Quddus, William Lewis, Robert A. Stockman Abstract In order to address the current downturn...

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In vitro and in vivo antifungal profile of a novel and long-acting inhaled azole, PC945, on Aspergillus fumigatus infection

Colley T., Alanio A., Kelly S.L., Sehra G., Kizawa Y., Warrilow A.G.S., Parker J.E., Kelly D.E., Kimura G., Anderson-Dring L., Nakaoki T., Sunose M., Onions S., Crepin D., Lagasse F., Crittall M., Shannon J.,...

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Discovery of novel benzothienoazepine derivatives as potent inhibitors of respiratory syncytial virus

Euan A.F. Fordyce, Daniel W. Brookes, Claire-Lise Ciana, Matthew S. Coates, S. Fraser Hunt, Kazuhiro Ito, John King-Underwood, Stuart T. Onions, Guillaume F. Parra, Garth Rapeport, Vladimir Sherbukhin, Jennifer A. Stockwell, Peter Strong, Jennifer...

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Synthesis of 4-​aminotetrahydropyran scaffolds for drug discovery

Andrew Nortcliffe, Gavin D.S. Milne, Daniel Hamza, Christopher J. Moody Abstract Functionalised tetrahydropyran scaffolds were prepared using a tethered enol-ether Prins cyclisation and elaborated to show their potential use in library synthesis. The key...

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Design and synthesis of a potent, highly selective, orally bioavailable, retinoic acid receptor alpha agonist

Clarke E., Jarvis C.I., Goncalves M.B., Kalindjian S.B., Adams D.R., Brown J.T., Shiers J.J., Taddei D.M.A., Ravier E., Barlow S., Miller I., Smith V., Borthwick A.D., Corcoran J.P.T. Abstract A ligand-based virtual screening exercise...

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Synthesis of Epibatidine Analogues by Pyrrole Diels-​Alder Reactions: Rapid Access to Azabicyclo[2.2.1]​heptane and 3,​8-​Diazabicyclo[3.2.1]​octane Scaffolds for Library Synthesis

Alexander T. Murray, Emma Packard, Andrew Nortcliffe, William Lewis, Daniel Hamza, Geraint Jones, Christopher J. Moody Abstract Analogues of the nicotinic acetylcholine antagonist epibatidine, suitable for diversification, were synthesized by application of a pyrrole...

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Combining two-directional synthesis and tandem reactions – Part 21: Exploitation of a dimeric macrocycle for chain terminus differentiation and synthesis of an sp3-rich library

Thomas E .Storra, Sarah J. Cully, Michael J. Rawling, William Lewis, Daniel Hamza, Geraint Jones, Robert A. Stockman Abstract The application of a tandem condensation/cyclisation/-cycloaddition/elimination reaction gives an sp3-rich tricyclic pyrazoline scaffold with two...

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Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2

Authors: Tom D. Heightman et al J. Med. Chem., Article ASAP DOI: 10.1021/acs.jmedchem.8b00421 Publication Date (Web): May 18, 2018 https://pubs.acs.org/doi/10.1021/acs.jmedchem.8b00421 Abstract Aberrant activation of the MAPK pathway drives cell proliferation in multiple cancers. Inhibitors of...

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