Search Results - "Bamford, Mark J"

Partial Reduction of Pyridinium Salts as a Versatile Route to Dihydropyridones by Donohoe, Timothy J., Johnson, Dale J., Mace, Laura H., Bamford, Mark J., Ichihara, Osamu

“…The addition of two electrons to a pyridinium salt turns it into a nucleophile. The intermediate generated by the reduction of such salts can be reacted…”
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GSK137, a potent small-molecule BCL6 inhibitor with in vivo activity, suppresses antibody responses in mice by Pearce, Andrew C., Bamford, Mark J., Barber, Ruth, Bridges, Angela, Convery, Maire A., Demetriou, Constantinos, Evans, Sian, Gobbetti, Thomas, Hirst, David J., Holmes, Duncan S., Hutchinson, Jonathan P., Jayne, Sandrine, Lezina, Larissa, McCabe, Michael T., Messenger, Cassie, Morley, Joanne, Musso, Melissa C., Scott-Stevens, Paul, Manso, Ana Sousa, Schofield, Jennifer, Slocombe, Tom, Somers, Don, Walker, Ann L., Wyce, Anastasia, Zhang, Xi-Ping, Wagner, Simon D.

“…B-cell lymphoma 6 (BCL6) is a zinc finger transcriptional repressor possessing a BTB–POZ (BR-C, ttk, and bab for BTB; pox virus and zinc finger for POZ)…”
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In search of a small molecule agonist of the relaxin receptor RXFP1 for the treatment of liver fibrosis by McBride, Andrew, Hoy, Anna M., Bamford, Mark J., Mossakowska, Danuta E., Ruediger, Martin P., Griggs, Jeremy, Desai, Sapna, Simpson, Kate, Caballero-Hernandez, Ivan, Iredale, John P., Pell, Theresa, Aucott, Rebecca L., Holmes, Duncan S., Webster, Scott P., Fallowfield, Jonathan A.

“…The peptide hormone human relaxin-2 (H2-RLX) has emerged as a potential therapy for cardiovascular and fibrotic diseases, but its short in vivo half-life is an…”
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Iridium-catalyzed formylation of amines with paraformaldehyde by Saidi, Ourida, Bamford, Mark J., Blacker, A. John, Lynch, James, Marsden, Stephen P., Plucinski, Pawel, Watson, Robert J., Williams, Jonathan M.J.

“…The reaction of amines with either formaldehyde or paraformaldehyde in water in the presence of [Cp∗IrI 2] 2 affords the corresponding formamides in good…”
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Copper-catalyzed rearrangement of oximes into primary amides by Sharma, Sumeet K., Bishopp, Simon D., Liana Allen, C., Lawrence, Ruth, Bamford, Mark J., Lapkin, Alexei A., Plucinski, Pawel, Watson, Robert J., Williams, Jonathan M.J.

“…The atom-efficient and cost-effective rearrangement of oximes into primary amides is catalyzed by simple copper salts. The use of homogeneous Cu(OAc)2…”
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Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes by Angell, Richard M., Angell, Tony D., Bamborough, Paul, Bamford, Mark J., Chung, Chun-wa, Cockerill, Stuart G., Flack, Stephen S., Jones, Katherine L., Laine, Dramane I., Longstaff, Timothy, Ludbrook, Steve, Pearson, Rosannah, Smith, Kathryn J., Smee, Penny A., Somers, Don O., Walker, Ann L.

“…The biphenyl amides (BPAs) are a series of p38α MAP kinase inhibitors. Compounds are able to bind to the kinase in either the DFG-in or DFG-out conformation,…”
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Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists by Wilson, David M., Apps, James, Bailey, Nicholas, Bamford, Mark J., Beresford, Isabel J., Brackenborough, Kim, Briggs, Michael A., Brough, Stephen, Calver, Andrew R., Crook, Barry, Davis, Rebecca K., Davis, Robert P., Davis, Susannah, Dean, David K., Harris, Leanne, Heslop, Teresa, Holland, Vicky, Jeffrey, Phillip, Panchal, Terrance A., Parr, Christopher A., Quashie, Nigel, Schogger, Joanne, Sehmi, Sanjeet S., Stean, Tania O., Steadman, Jon G.A., Trail, Brenda, Wald, Jeffrey, Worby, Angela, Takle, Andrew K., Witherington, Jason, Medhurst, Andrew D.

“…This Letter describes the discovery of GSK189254 and GSK239512 that were progressed as clinical candidates to explore the potential of H3 receptor antagonists…”
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The discovery of the benzazepine class of histamine H3 receptor antagonists by Wilson, David M., Apps, James, Bailey, Nicholas, Bamford, Mark J., Beresford, Isabel J., Briggs, Michael A., Calver, Andrew R., Crook, Barry, Davis, Robert P., Davis, Susannah, Dean, David K., Harris, Leanne, Heightman, Tom D., Panchal, Terry, Parr, Christopher A., Quashie, Nigel, Steadman, Jon G.A., Schogger, Joanne, Sehmi, Sanjeet S., Stean, Tania O., Takle, Andrew K., Trail, Brenda K., White, Trevor, Witherington, Jason, Worby, Angela, Medhurst, Andrew D.

“…This Letter describes the discovery of a novel series of H3 receptor antagonists. The initial medicinal chemistry strategy focused on deconstructing and…”
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Orally active C-6 heteroaryl- and heterocyclyl-substituted imidazo[1,2- a]pyridine acid pump antagonists (APAs) by Bailey, Nick, Bamford, Mark J., Brissy, Delphine, Brookfield, Joanna, Demont, Emmanuel, Elliott, Richard, Garton, Neil, Farre-Gutierrez, Irene, Hayhow, Thomas, Hutley, Gail, Naylor, Antoinette, Panchal, Terry A., Seow, Hui-Xian, Spalding, David, Takle, Andrew K.

“…A series of novel imidazo[1,2- a]pyridine acid pump antagonists is described. Heteroaryl and heterocyclic substituents at the C-6 position were used for the…”
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The identification of potent, selective and CNS penetrant furan-based inhibitors of B-Raf kinase by Takle, Andrew K., Bamford, Mark J., Davies, Susannah, Davis, Robert P., Dean, David K., Gaiba, Alessandra, Irving, Elaine A., King, Frank D., Naylor, Antoinette, Parr, Christopher A., Ray, Alison M., Reith, Alastair D., Smith, Beverley B., Staton, Penelope C., Steadman, Jon G.A., Stean, Tania O., Wilson, David M.

“…Modification of the potent imidazole-based B-Raf inhibitor SB-590885 resulted in the identification of a series of furan-based derivatives with enhanced CNS…”
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(1 H-Imidazo[4,5- c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: A novel class of potent MSK-1-inhibitors by Bamford, Mark J., Alberti, Michael J., Bailey, Nicholas, Davies, Susannah, Dean, David K., Gaiba, Alessandra, Garland, Stephen, Harling, John D., Jung, David K., Panchal, Terence A., Parr, Christopher A., Steadman, Jon G., Takle, Andrew K., Townsend, James T., Wilson, David M., Witherington, Jason

“…A novel series of imidazo[4,5- c]pyridines bearing a 1,2,5-oxadiazol-3-ylamine functionality has been developed. These are potent inhibitors of mitogen and…”
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Synthesis and antiviral activity of 3'-deoxy-3'-C-hydroxymethyl nucleosides by Bamford, Mark J, Coe, Paul L, Walker, Richard T

“…A series of 3'-branched-chain sugar nucleosides, in particular 3'-deoxy-3'-C-hydroxmethyl nucleosides, have been synthesized and evaluated as antiviral agents…”
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(1 H-Imidazo[4,5- c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: Further optimisation as highly potent and selective MSK-1-inhibitors by Bamford, Mark J., Bailey, Nicholas, Davies, Susannah, Dean, David K., Francis, Leann, Panchal, Terence A., Parr, Christopher A., Sehmi, Sanjeet, Steadman, Jon G., Takle, Andrew K., Townsend, James T., Wilson, David M.

“…The novel imidazo[4,5- c]pyridine 1,2,5-oxadiazol-3-yl template affords an excellent start point for identification of inhibitors of a number of protein…”
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The ammonia-free partial reduction of substituted pyridinium salts by Donohoe, Timothy J, Johnson, Dale J, Mace, Laura H, Thomas, Rhian E, Chiu, Jessica Y K, Rodrigues, Jason S, Compton, Richard G, Banks, Craig E, Tomcik, Peter, Bamford, Mark J, Ichihara, Osamu

“…This paper reports a study into the partial reduction of N-alkylpyridinium salts together with subsequent elaboration of the intermediates thus produced…”
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4-Acyl-1-(4-aminoalkoxyphenyl)-2-ketopiperazines as a Novel Class of Non-Brain-Penetrant Histamine H3 Receptor Antagonists by Procopiou, Panayiotis A, Ancliff, Rachael A, Bamford, Mark J, Browning, Christopher, Connor, Helen, Davies, Susannah, Fogden, Yvonne C, Hodgson, Simon T, Holmes, Duncan S, Looker, Brian E, Morriss, Karen M. L, Parr, Christopher A, Pickup, Elizabeth A, Sehmi, Sanjeet S, White, Gemma V, Watts, Clarissa J, Wilson, David M, Woodrow, Michael D

“…A series of ketopiperazines were prepared and evaluated for their activity as histamine H3 antagonists. From investigation of the tertiary basic center in the…”
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Synthesis and antiviral activity of some 3'-C-difluoromethyl- and 3'-deoxy-3'-C-fluoromethyl nucleosides by Bamford, Mark J, Coe, Paul L, Walker, Richard T

“…The synthesis and antiviral activity of a number of 3'-C-difluoromethyl and 3'-deoxy-3'-C-fluoromethyl nucleosides are reported. The 3'-C-difluoromethyl…”
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Functionalised pyrrolidinones derived from ( S)-pyroglutamic acid by Beard, Mark J, Bailey, Jonathan H, Cherry, David T, Moloney, Mark G, Shim, Sung Bo, Statham, Kathryn A, Bamford, Mark J, Brian Lamont, R

“…The generation of the lactam enolate derived from bicyclic lactams 2a-c, prepared from ( S)-pyroglutamic acid 1a, and subsequent reaction with a range of…”
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A concise approach to functionalised, homochiral pyrrolidinones by Bamford, Mark J, Beard, Mark, Cherry, David T, Moloney, Mark G

“…Acylation of O, N-acetal 1 gives excellent yields of the C-7 substituted products 2a,b. Alkylation of 2a under mild conditions gives high yields of the exo- 3…”
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A series of penicillin-derived C2-symmetric inhibitors of HIV-1 proteinase: synthesis, mode of interaction, and structure-activity relationships by Humber, David C, Bamford, Mark J, Bethell, Richard C, Cammack, Nicholas, Cobley, Kevin, Evans, Derek N, Gray, Norman M, Hann, Michael M, Orr, David C

“…The C2-symmetric diester 1 was identified by random screening as a novel inhibitor of HIV-1 proteinase. This led to the preparation of a series of related more…”
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Corrigendum to “(1H-Imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: A novel class of potent MSK-1-inhibitors” [Bioorg. Med. Chem. Lett. 15 (2005) 3402–3406] by Bamford, Mark J., Alberti, Michael J., Bailey, Nicholas, Davies, Susannah, Dean, David K., Gaiba, Alessandra, Garland, Stephen, Harling, John D., Jung, David K., Panchal, Terence A., Parr, Christopher A., Steadman, Jon G., Takle, Andrew K., Townsend, James T., Wilson, David M., Witherington, Jason

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