Search Results - "Jones, Clifford D."

Sustained Mps1 activity is required in mitosis to recruit O-Mad2 to the Mad1–C-Mad2 core complex by Hewitt, Laura, Tighe, Anthony, Santaguida, Stefano, White, Anne M., Jones, Clifford D., Musacchio, Andrea, Green, Stephen, Taylor, Stephen S.

“…Mps1 is an essential component of the spindle assembly checkpoint. In this study, we describe a novel Mps1 inhibitor, AZ3146, and use it to probe the role of…”
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Cellularly active N-hydroxyurea FEN1 inhibitors block substrate entry to the active site by Exell, Jack C, Thompson, Mark J, Finger, L David, Shaw, Steven J, Debreczeni, Judit, Ward, Thomas A, McWhirter, Claire, Siöberg, Catrine L B, Molina, Daniel Martinez, Abbott, W Mark, Jones, Clifford D, Nissink, J Willem M, Durant, Stephen T, Grasby, Jane A

“…Structural, enzymatic and cellular target engagement studies reveal the mechanism of action by N -hydroxyurea small molecule inhibitors of the DNA repair…”
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Cell-Active Small Molecule Inhibitors of the DNA-Damage Repair Enzyme Poly(ADP-ribose) Glycohydrolase (PARG): Discovery and Optimization of Orally Bioavailable Quinazolinedione Sulfonamides by Waszkowycz, Bohdan, Smith, Kate M, McGonagle, Alison E, Jordan, Allan M, Acton, Ben, Fairweather, Emma E, Griffiths, Louise A, Hamilton, Niall M, Hamilton, Nicola S, Hitchin, James R, Hutton, Colin P, James, Dominic I, Jones, Clifford D, Jones, Stuart, Mould, Daniel P, Small, Helen F, Stowell, Alexandra I. J, Tucker, Julie A, Waddell, Ian D, Ogilvie, Donald J

“…DNA damage repair enzymes are promising targets in the development of new therapeutic agents for a wide range of cancers and potentially other diseases. The…”
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The discovery of AZD5597, a potent imidazole pyrimidine amide CDK inhibitor suitable for intravenous dosing by Jones, Clifford D., Andrews, David M., Barker, Andrew J., Blades, Kevin, Daunt, Paula, East, Simon, Geh, Catherine, Graham, Mark A., Johnson, Keith M., Loddick, Sarah A., McFarland, Heather M., McGregor, Alexandra, Moss, Louise, Rudge, David A., Simpson, Peter B., Swain, Michael L., Tam, Kin Y., Tucker, Julie A., Walker, Mike

“…Describes the optimisation of an imidazole amide series, leading to the identification of ( S)- 15b (AZD5597) as a candidate for further development. The…”
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Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC) by Ward, Richard A, Anderton, Mark J, Bethel, Paul, Breed, Jason, Cook, Calum, Davies, Emma J, Dobson, Andrew, Dong, Zhiqiang, Fairley, Gary, Farrington, Paul, Feron, Lyman, Flemington, Vikki, Gibbons, Francis D, Graham, Mark A, Greenwood, Ryan, Hanson, Lyndsey, Hopcroft, Philip, Howells, Rachel, Hudson, Julian, James, Michael, Jones, Clifford D, Jones, Christopher R, Li, Yongchao, Lamont, Scott, Lewis, Richard, Lindsay, Nicola, McCabe, James, McGuire, Thomas, Rawlins, Philip, Roberts, Karen, Sandin, Linda, Simpson, Iain, Swallow, Steve, Tang, Jia, Tomkinson, Gary, Tonge, Michael, Wang, Zhenhua, Zhai, Baochang

“…The RAS/MAPK pathway is a major driver of oncogenesis and is dysregulated in approximately 30% of human cancers, primarily by mutations in the BRAF or RAS…”
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Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2 by Ward, Richard A, Colclough, Nicola, Challinor, Mairi, Debreczeni, Judit E, Eckersley, Kay, Fairley, Gary, Feron, Lyman, Flemington, Vikki, Graham, Mark A, Greenwood, Ryan, Hopcroft, Philip, Howard, Tina D, James, Michael, Jones, Clifford D, Jones, Christopher R, Renshaw, Jonathan, Roberts, Karen, Snow, Lindsay, Tonge, Michael, Yeung, Kay

“…The RAS/RAF/MEK/ERK signaling pathway has been targeted with a number of small molecule inhibitors in oncology clinical development across multiple disease…”
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AZD0364 Is a Potent and Selective ERK1/2 Inhibitor That Enhances Antitumor Activity in KRAS -Mutant Tumor Models when Combined with the MEK Inhibitor, Selumetinib by Flemington, Vikki, Davies, Emma J, Robinson, David, Sandin, Linda C, Delpuech, Oona, Zhang, Pei, Hanson, Lyndsey, Farrington, Paul, Bell, Sigourney, Falenta, Katarzyna, Gibbons, Francis D, Lindsay, Nicola, Smith, Aaron, Wilson, Joanne, Roberts, Karen, Tonge, Michael, Hopcroft, Philip, Willis, Sophie E, Roudier, Martine P, Rooney, Claire, Coker, Elizabeth A, Jaaks, Patricia, Garnett, Mathew J, Fawell, Stephen E, Jones, Clifford D, Ward, Richard A, Simpson, Iain, Cosulich, Sabina C, Pease, J Elizabeth, Smith, Paul D

“…The RAS-regulated RAF-MEK1/2-ERK1/2 (RAS/MAPK) signaling pathway is a major driver in oncogenesis and is frequently dysregulated in human cancers, primarily by…”
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Structure-Guided Discovery of Potent and Selective Inhibitors of ERK1/2 from a Modestly Active and Promiscuous Chemical Start Point by Ward, Richard A, Bethel, Paul, Cook, Calum, Davies, Emma, Debreczeni, Judit E, Fairley, Gary, Feron, Lyman, Flemington, Vikki, Graham, Mark A, Greenwood, Ryan, Griffin, Nicola, Hanson, Lyndsey, Hopcroft, Philip, Howard, Tina D, Hudson, Julian, James, Michael, Jones, Clifford D, Jones, Christopher R, Lamont, Scott, Lewis, Richard, Lindsay, Nicola, Roberts, Karen, Simpson, Iain, St-Gallay, Steve, Swallow, Steve, Tang, Jia, Tonge, Michael, Wang, Zhenhua, Zhai, Baochang

“…There are a number of small-molecule inhibitors targeting the RAS/RAF/MEK/ERK signaling pathway that have either been approved or are in clinical development…”
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Discovery of a Potent, Selective, Orally Bioavailable, and Efficacious Novel 2‑(Pyrazol-4-ylamino)-pyrimidine Inhibitor of the Insulin-like Growth Factor‑1 Receptor (IGF-1R) by Degorce, Sébastien L, Boyd, Scott, Curwen, Jon O, Ducray, Richard, Halsall, Christopher T, Jones, Clifford D, Lach, Franck, Lenz, Eva M, Pass, Martin, Pass, Sarah, Trigwell, Catherine

“…Optimization of cellular lipophilic ligand efficiency (LLE) in a series of 2-anilino-pyrimidine IGF-1R kinase inhibitors led to the identification of novel…”
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Novel imidazo[1,2-a]pyridine based inhibitors of the IGF-1 receptor tyrosine kinase: Optimization of the aniline by Ducray, Richard, Jones, Clifford D., Jung, Frederic H., Simpson, Iain, Curwen, Jon, Pass, Martin

“…Following the discovery of imidazopyridine 1 as a potent IGF-1R tyrosine kinase inhibitor, the aniline part has been modified with the aim to optimize the…”
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The Wnt Pathway Inhibitor RXC004 Blocks Tumor Growth and Reverses Immune Evasion in Wnt Ligand-dependent Cancer Models by Phillips, Caroline, Bhamra, Inder, Eagle, Catherine, Flanagan, Eimear, Armer, Richard, Jones, Clifford D, Bingham, Matilda, Calcraft, Peter, Edmenson Cook, Alicia, Thompson, Ben, Woodcock, Simon A

“…Wnt signaling is implicated in the etiology of gastrointestinal tract cancers. Targeting Wnt signaling is challenging due to on-target toxicity concerns and…”
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Novel and Versatile Synthesis of Disubstituted 1,2-Dihydro-1,2,4-triazol-3-ones by Graham, Mark A, Bethel, Paul A, Burgess, Jonathan, Fairley, Gary, Glossop, Steve C, Greenwood, Ryan D. R, Jones, Clifford D, Lovell, Scott, Swallow, Steve

“…A novel method for the synthesis of a wide range of 1,5-disubstituted 1,2-dihydro-1,2,4-triazol-3-ones is described. The key step involves a reaction between a…”
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Design of a potent, soluble glucokinase activator with excellent in vivo efficacy by McKerrecher, Darren, Allen, Joanne V., Caulkett, Peter W.R., Donald, Craig S., Fenwick, Mark L., Grange, Emma, Johnson, Keith M., Johnstone, Craig, Jones, Clifford D., Pike, Kurt G., Rayner, John W., Walker, Rolf P.

“…The optimisation of a series of glucokinase activators is described, including attempts to uncouple the relationship between potency and plasma protein…”
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Two-Directional Approach for the Rapid Synthesis of 2,4-Bis-Aminoaryl Pyridine Derivatives by Morgentin, Rémy, Barlaam, Bernard, Foote, Kevin, Hassall, Lorraine, Hawkins, Janet, Jones, Clifford D., Le Griffon, Antoine, Peru, Aurelien, Plé, Patrick

“…We have developed two different approaches in parallel to rapidly access 2,4-bis aminoaryl pyridine compounds from a common starting material. The C-4/C-2…”
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Abstract 3343: The pre-clinical in vitro and in vivo activity of AZD6738: A potent and selective inhibitor of ATR kinase by Guichard, Sylvie M., Brown, Elaine, Odedra, Rajesh, Hughes, Adina, Heathcote, Dan, Barnes, Jen, Lau, Alan, Powell, Steve, Jones, Clifford D., Nissink, Willem, Foote, Kevin M., Jewsbury, Philip J., Pass, Martin

“…Abstract AZD6738 is a potent and selective orally bioavailable kinase inhibitor of ataxia telangiectasia and rad3 related (ATR). Here we report the…”
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Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors by Jones, Clifford D., Andrews, David M., Barker, Andrew J., Blades, Kevin, Byth, Kate F., Finlay, M. Raymond V., Geh, Catherine, Green, Clive P., Johannsen, Marie, Walker, Mike, Weir, Hazel M.

“…The SAR and optimisation of a novel series of imidazole pyrimidine amides is reported. The development of a novel series of imidazole pyrimidine amides as…”
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Unusual reactivity of N-acyl imides: N-aroyl-1,2,4-dithiazolidine-3,5-diones as acyl isocyanate equivalents by Wood, Mark E, Annis, Victoria M, Jones, Clifford D

“…Crystalline samples of three N-aroyl-1,2,4-dithiazolidine-3,5-diones have been prepared as the first examples of a novel class of compound that displays the…”
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Discovery, synthesis and biological evaluation of novel glucokinase activators by McKerrecher, Darren, Allen, Joanne V., Bowker, Suzanne S., Boyd, Scott, Caulkett, Peter W.R., Currie, Gordon S., Davies, Christopher D., Fenwick, Mark L., Gaskin, Harold, Grange, Emma, Hargreaves, Rod B., Hayter, Barry R., James, Roger, Johnson, Keith M., Johnstone, Craig, Jones, Clifford D., Lackie, Sarah, Rayner, John W., Walker, Rolf P.

“…[Display omitted] The identification, synthesis and SAR of a novel series of glucokinase activators is described. The interplay between lipophilicity, potency…”
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Asymmetric synthesis of epibatidine by use of a novel enantioselective sulfinate elimination reaction by Jones, Clifford D., Simpkins, Nigel S., Giblin, Gerard M.P.

“…A vicinal bis-sulfone having the 7-azabicyclo[2.2.1]heptane skeleton undergoes a novel type of asymmetric elimination on treatment with the sodium alkoxide…”
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REDX12271 Is a Novel, Selective DDR1 Inhibitor With the Potential to Treat Multiple Chronic Kidney Diseases: TH-PO433 by Eckersley, Kay, Bhamra, Inder, Ryan, James, Andrae, Michal S., Wilcock, Daniel J., Preece, Shân, Bunyard, Peter R., Jones, Clifford D., Armer, Richard

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