Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Kenneth Wiggall"'
Autor:
Nannan Liu, Michael N. Zimmerman, Richard M. Keenan, Victor K. Johnston, Deping Chai, Rosanna Tedesco, Duke M. Fitch, Juili Lin-Goerke, Kenneth Wiggall, Antony N. Shaw, Nestor O. Concha, Ramesh Bambal, Michael G. Darcy, Robert T. Sarisky, Dashyant Dhanak, Kevin J. Duffy, Adam T. Gates
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4350-4353
The synthesis and optimisation of HCV NS5B polymerase inhibitors with improved potency versus the existing compound 1 is described. Substitution in the benzothiadiazine portion of the molecule, furnishing improvement in potency in the high protein Re
Autor:
Britta Will, Beth Pietrak, Maria Faelth-Savitski, Nicholas D. Adams, Kelly Mitchell, Arthur Groy, Jessy Cartier, Alan R. Rendina, Yun Ruei Kao, Enoch Gao, Nestor O. Concha, Laura Barreyro, Gerard Drewes, Huizhen Zhao, Kenneth Wiggall, Pat Brady, Hideki Makishima, Jaroslaw P. Maciejewski, Chaya Duraiswami, Heng Rui Wang, Cynthia M. Rominger, Iléana Antony-Debré, Maximilian Christopeit, Ulrich Steidl, Elisabeth Paietta, Chad Quinn, Luis A. Carvajal, Marcus Bantscheff, Alexander Joseph Reif, Ujunwa C. Okoye-Okafor, Schmidt Stanley J, Boris Bartholdy, Hongwei Qi, Benjamin Schwartz, Gerard Joberty, Swathi Rao Narayanagari, Amit Verma, Angela Smallwood, Michael T. McCabe
Publikováno v:
Nature chemical biology. 11(11)
Neomorphic mutations in isocitrate dehydrogenase 1 (IDH1) are driver mutations in acute myeloid leukemia (AML) and other cancers. We report the development of new allosteric inhibitors of mutant IDH1. Crystallographic and biochemical results demonstr
Autor:
Chao Han, Warren W. Gerhardt, Dashyant Dhanak, Kevin J. Duffy, Nestor O. Concha, Adam T. Gates, Richard M. Keenan, Victor K. Johnston, Glenn A. Hofmann, Duke M. Fitch, Nannan Liu, Kenneth Wiggall, Antony N. Shaw, Dina L. Halegoua, Robert T. Sarisky, Michael N. Zimmerman, Ramesh Bambal, Michael G. Darcy, Arun C. Kaura, Juili Lin-Goerke, Deping Chai, Rosanna Tedesco
Publikováno v:
Journal of Medicinal Chemistry. 49:971-983
Recently, we disclosed a new class of HCV polymerase inhibitors discovered through high-throughput screening (HTS) of the GlaxoSmithKline proprietary compound collection. This interesting class of 3-(1,1-dioxo-2H-1,2,4-benzothiadiazin-3-yl)-4-hydroxy
Autor:
Kenneth Wiggall, Lihua Zhang, Heather Smith, Peter Lamb, Evelyne Delorme, Susan B. Dillon, Shaw Antony N, Richard M. Keenan, Celine Duquenne, Connie L. Erickson-Miller, Yifang Huang, Nannan Liu, Kevin J. Duffy, Stephen G. Miller, Price Alan T, Leslie Giampa, Juan I. Luengo, Jon Rosen
Publikováno v:
Journal of Medicinal Chemistry. 45:3576-3578
The invention of a new class of naphtho[1,2-d]imidazole thrombopoietin mimics based on a pharmacophore hypothesis for small-molecule thrombopoietic agonists is discussed. Parallel array synthesis and purification techniques allowed for the rapid expl
Autor:
Leach Colin Andrew, David R. Reavill, Kenneth Wiggall, Colin J. Theobald, David J. Keeling, Robert John Ife, Thomas Henry Brown, Malcolm L. Meeson, Michael E. Parsons
Publikováno v:
Journal of Medicinal Chemistry. 35:3413-3422
Previously, gastric (H+/K+)-ATPase inhibitors such as 2 have been prepared as analogues of 1a on the presumption that the 3-carbethoxy substituent plays a key role in establishing the orientation of the 4-arylamino group. In this paper we explore fur
Autor:
Michael E. Parsons, Leach Colin Andrew, Kenneth Wiggall, David J. Keeling, Thomas Henry Brown, Carolyn A. Price, Shiona M. Laing, Robert John Ife
Publikováno v:
Journal of Medicinal Chemistry. 35:1845-1852
Further work on compounds 1 has identified the 4-position as a site where substantial modifications are tolerated, leading to analogues which are more potent and less toxic than those described previously. The best compound in the series is 13a (SK&F
Autor:
Rosanna Tedesco, Duke M. Fitch, Robert T. Sarisky, Antony N. Shaw, Michael N. Zimmerman, Kevin J. Duffy, Michael G. Darcy, Dashyant Dhanak, Juili Lin-Goerke, Richard M. Keenan, Adam T. Gates, Victor K. Johnston, Deping Chai, Kenneth Wiggall, Klára Valkó
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(15)
Modification of the benzo rings of 3-(1,1-dioxo-2H-(1,2,4)-benzothiadiazin-3-yl)-4-hydroxy-2(1H)-quinolinones into heteroaromatic systems was investigated to enhance physicochemical properties and potency profile of this class of inhibitors. The synt
Autor:
Stephen G. Miller, Price Alan T, Daniel F. Eppley, Jon Rosen, Nannan Liu, Evelyne Delorme, Kevin J. Duffy, Peter Lamb, Richard M. Keenan, Kenneth Wiggall, Lynnette Leong, Rakhi Shah, Kenneth C. Stark, Leslie Giampa, Curtis M. Tyree, Yifang Huang, Shin-Shay Tian, Juan I. Luengo, Susan B. Dillon, Tony Shaw, Heather Smith, Michael G. Darcy, Lily Zhang, Christopher B. Hopson, Connie L. Erickson-Miller
Publikováno v:
Journal of medicinal chemistry. 44(22)
High-throughput screening for the induction of a luciferase reporter gene in a thrombopoietin (TPO)-responsive cell line resulted in the identification of 4-diazo-3-hydroxy-1-naphthalenesulfonic acids as TPO mimics. Modification of the core structure
Autor:
Robert John Ife, Leach Colin Andrew, Kenneth Wiggall, Thomas Henry Brown, Michael E. Parsons, Colin J. Theobald, David J. Keeling
Publikováno v:
Journal of medicinal chemistry. 38(14)
3-Acyl-4-(arylamino)quinolines were previously identified as gastric (H + /K + )-ATPase inhibitors, and clinical efficacy has been demonstrated for compound 3 (SK&F 96067). In the present study the further structure-activity relationship of this seri
Autor:
Leach Colin Andrew, Kenneth Wiggall, David R. Reavill, David J. Keeling, Shiona M. Laing, Thomas Henry Brown, Robert John Ife, Michael E. Parsons, Carolyn A. Price
Publikováno v:
Journal of medicinal chemistry. 33(2)
The 4-(arylamino)quinoline 4, previously described as an antiulcer compound, is shown to be an inhibitor of the gastric (H+/K+)-ATPase. It is postulated that 1-arylpyrrolo[3,2-c]quinolines 6 act as conformationally restrained analogues of 4. A series