Search Results - "Teague, Simon J"

Implications of protein flexibility for drug discovery by Teague, Simon J

“…Proteins are in constant motion between different conformational states with similar energies. This has often been ignored in drug design. However, protein…”
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Synthesis of Heavily Substituted 2-Aminopyridines by Displacement of a 6-Methylsulfinyl Group by Teague, Simon J

“…2-Aminopyridines, with a variety of polar 6-substituents, were elaborated by displacement of a methylsulfinyl group from the 6-position of the pyridine ring…”
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Application and Limitations of X-ray Crystallographic Data in Structure-Based Ligand and Drug Design by Davis, Andrew M., Teague, Simon J., Kleywegt, Gerard J.

“…Structure‐based design usually focuses upon the optimization of ligand affinity. However, successful drug design also requires the optimization of many other…”
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Learning lessons from drugs that have recently entered the market by Teague, Simon J.

“…Which projects in the drug discovery field are most likely to be successful? In this article, I provide guidelines for answering this question by examining…”
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Concrete evidence of confusion by Teague, Simon J

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Euodenine A: A Small-Molecule Agonist of Human TLR4 by Neve, Juliette E, Wijesekera, Hasanthi P, Duffy, Sandra, Jenkins, Ian D, Ripper, Justin A, Teague, Simon J, Campitelli, Marc, Garavelas, Agatha, Nikolakopoulos, George, Le, Phuc V, de A. Leone, Priscila, Pham, Ngoc B, Shelton, Philip, Fraser, Neil, Carroll, Anthony R, Avery, Vicky M, McCrae, Christopher, Williams, Nicola, Quinn, Ronald J

“…A small-molecule natural product, euodenine A (1), was identified as an agonist of the human TLR4 receptor. Euodenine A was isolated from the leaves of Euodia…”
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The Design of Leadlike Combinatorial Libraries by Teague, Simon J., Davis, Andrew M., Leeson, Paul D., Oprea, Tudor

“…The optimization of low‐potency leads into drugs is often accompanied by an increase in molecular weight (Mr) and lipophilicity, as a consequence of affinity…”
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Synthesis of melicodenines C, D and E by Holla, Harish, Jenkins, Ian D., Neve, Juliette E., Pouwer, Rebecca H., Pham, Ngoc, Teague, Simon J., Quinn, Ronald J.

“…A synthesis of the unusual cyclobutane-quinolinone alkaloids melicodenines C, D and E by intermolecular [2+2] cycloaddition is described…”
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Is There a Difference between Leads and Drugs? A Historical Perspective by Oprea, Tudor I, Davis, Andrew M, Teague, Simon J, Leeson, Paul D

“…To be considered for further development, lead structures should display the following properties:  (1) simple chemical features, amenable for chemistry…”
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Hydrogen Bonding, Hydrophobic Interactions, and Failure of the Rigid Receptor Hypothesis by Davis, Andrew M., Teague, Simon J.

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Discovery of potent CRTh2 (DP 2) receptor antagonists by Birkinshaw, Timothy N., Teague, Simon J., Beech, Claire, Bonnert, Roger V., Hill, Stephen, Patel, Anil, Reakes, Sara, Sanganee, Hitesh, Dougall, Iain G., Phillips, Tim T., Salter, Sylvia, Schmidt, Jerzy, Arrowsmith, Elizabeth C., Carrillo, Juan J., Bell, Fiona M., Paine, Stuart W., Weaver, Richard

“…The discovery and optimisation of potent antagonists of the CRTh2 receptor is described culminating in the synthesis of 12, a novel, potent, selective and…”
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Facile synthesis of a o-nitrobenzyl photolabile linker for combinatorial chemistry by Teague, Simon J

“…Two facile syntheses are described of the o-nitrobenzyl alcohol photolabile linker ( 5). This compound is a valuable intermediate in the preparation of…”
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Solid-Phase Total Synthesis of Oscillamide Y and Analogues by Marsh, Ian R, Bradley, Mark, Teague, Simon J

“…We report an efficient solid phase synthesis of oscillamide Y and three analogues. The cyclic peptide was prepared using a combination of Fmoc and allyl…”
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Library synthesis using solution phase capping of solid phase derived intermediates by Teague, Simon J, Walters, Iain A.S

“…An efficient protocol for the preparation of combinatorial libraries is described. The methodology first deploys solid phase chemistry to synthesize a 96-well…”
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Hydrogen Bonding, Hydrophobic Interactions, and Failure of the Rigid Receptor Hypothesis by Davis, Andrew M., Teague, Simon J.

“…Why does experimental determination of the structure of drug–receptor complexes so often result in surprises? The importance of hydrogen bonding and…”
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Synthesis of 6-substituted 5-cyano-7-hydroxy-2-carboxybenzofurans by Teague, Simon J., Barber, Simon

“…Methods for the synthesis of 5-cyano-7-hydroxy-2-carboxybenzofurans bearing a variety of substituents at the 6-position are outlined. The scope and limitations…”
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Asymmetric total synthesis of (-)-podophyllotoxin by Andrews, Robert C., Teague, Simon J., Meyers, Albert I.

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Macrocyclic ring closures employing the Intramolecular Heck reaction by Stocks, Michael J., Harrison, Richard P., Teague, Simon J.

“…Intramolecular Heck reactions have been employed for the final ring closure step in the construction of a series of macrocyclic compounds. Intramolecular Heck…”
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Discovery and synthesis of methyl 2,5-dimethyl-4-[2-(phenylmethyl)benzoyl]-1H-pyrrole-3-carboxylate (FPL 64176) and analogs: the first examples of a new class of calcium channel activator by Baxter, Andrew J. G, Dixon, John, Ince, Francis, Manners, Carol N, Teague, Simon J

“…Methyl 2,5-dimethyl-4-[2-(phenylmethyl)benzoyl]-1H-pyrrole-3-carboxylate, FPL 64176 (1), is the first example of a new class of calcium channel activator (CCA)…”
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Synthesis of benzimidazole based JNK inhibitors by Teague, Simon J., Barber, Simon, King, Sarah, Stein, Linda

“…Substituted benzimidazoles were synthesised using a number of novel reactions, including displacement of a 2-sulfone group, preparation of 4-diazo…”
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