Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Clement Douault"'
Autor:
Alex Preston, Scott McCleary, Emma J. Jones, Huw D. Lewis, Michael David Barker, Robert J. Watson, Tracy Jane Shipley, Cesar Ramirez-Molina, Dave Lugo, Clement Douault, Robert P. Davis, David Matthew Wilson, Margarete Neu, Neil Stuart Garton, Edward Hooper-Greenhill, John Liddle, Don O. Somers
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:4606-4612
The optimisation of the azanaphthyridine series of Spleen Tyrosine Kinase inhibitors is described. The medicinal chemistry strategy was focused on optimising the human whole blood activity whilst achieving a sufficient margin over hERG activity. A go
Autor:
Clement Douault, Tony Kouzarides, Robert J. Sheppard, Hawa Diallo, Paola Grandi, Samuel Robson, Chun-wa Chung, Ka Hing Che, Rab K. Prinjha, Richard J. Upton, Darren Jason Mitchell, Rebecca C. Furze, Emmanuel Hubert Demont, Andrew J. Bannister, Anne-Marie Michon, Robert J. Watson, Christina Rau, Paul Bamborough
Publikováno v:
Angew Chem Int Ed Engl
ATAD2 is a cancer-associated protein whose bromodomain has been described as among the least druggable of that target class. Starting from a potent lead, permeability and selectivity were improved through a dual approach: 1) using CF(2) as a sulfone
Autor:
Emma J. Jones, David P. Dixon, Robert J. Watson, Chun-wa Chung, Anne-Marie Michon, Clement Douault, Emmanuel Hubert Demont, Paul Bamborough, Hawa Diallo, Thilo Werner, Christina Rau, Paola Grandi, Robert J. Sheppard, Rab K. Prinjha, Rebecca C. Furze, Bhumika Karamshi, Darren Jason Mitchell, Heather A. Barnett
Publikováno v:
Journal of Medicinal Chemistry. 58:6151-6178
ATAD2 is a bromodomain-containing protein whose overexpression is linked to poor outcomes in a number of different cancer types. To date, no potent and selective inhibitors of the bromodomain have been reported. This article describes the structure-b
Autor:
Laurens Kruidenier, Rebecca Randle, Hawa Diallo, Inma Rioja, Clement Douault, Anne Rueger, Chun-wa Chung, Thomas George Christopher Hayhow, Rab K. Prinjha, Alex Preston, Roy Katso, Matthew Campbell, Michael David Barker, J. Mosley, Kevin Lee, Joanna Taylor, Marcel Muelbaier, Douglas W. Thomson, Gail A. Seal, Jack A. Brown, Susan Marie Westaway, Onkar M. P. Singh, Gerard Joberty, Philip G. Humphreys, Melanie Leveridge, Laurie J. Gordon, Pamela Thomas, Carl Haslam, Fiona Brown, John Liddle, Gerard Drewes, Robert Eagle, Robert J. Sheppard, David Matthew Wilson
Publikováno v:
Journal of medicinal chemistry. 59(4)
Optimization of KDM6B (JMJD3) HTS hit 12 led to the identification of 3-((furan-2-ylmethyl)amino)pyridine-4-carboxylic acid 34 and 3-(((3-methylthiophen-2-yl)methyl)amino)pyridine-4-carboxylic acid 39 that are inhibitors of the KDM4 (JMJD2) family of
Autor:
Philip Alan Skone, Donald O. Somers, Marion C. Dickson, Nick Smithers, Ann Louise Walker, Thomas George Christopher Hayhow, Stuart G. Leach, Karen Leavens, Clement Douault, Emma J. Jones, Dorothy Elwes, Robert J. Watson, Margarete Neu, Robert P. Davis, Matthew Gray, Neil Stuart Garton, Clare I. Hobbs, Alex Preston, Michael David Barker, Vipulkumar Kantibhai Patel, Cesar Ramirez-Molina, Paul S. Carter, Scott McCleary, Gordon G. Weingarten, Huw D. Lewis, Francis Louis Atkinson, John Liddle, Tracy Jane Shipley, Neil R. Curtis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6188-6194
The lead optimisation of the diaminopyrimidine carboxamide series of spleen tyrosine kinase inhibitors is described. The medicinal chemistry strategy was focused on optimising the human whole blood activity whilst achieving a sufficient margin over l
Autor:
Andrew D. Roberts, Bhumika Karamshi, Angela Bridges, Hawa Diallo, Chun-wa Chung, Kelly Locke, Peter D. Craggs, Darren Jason Mitchell, Paul Bamborough, Amanda Emmons, Christopher Roland Wellaway, Emma J. Jones, David P. Dixon, Robert J. Watson, Nathalie Barrett, Emmanuel Hubert Demont, Clement Douault, Robert J. Sheppard, Rab K. Prinjha, Rebecca C. Furze, Anne-Marie Michon, Paola Grandi, Bernadette Mouzon
Publikováno v:
Journal of medicinal chemistry. 58(14)
Overexpression of ATAD2 (ATPase family, AAA domain containing 2) has been linked to disease severity and progression in a wide range of cancers, and is implicated in the regulation of several drivers of cancer growth. Little is known of the dependenc
Autor:
Mark Patrick Healy, Karamjit S. Jandu, Kim L. Matthews, James E. Rowedder, Clement Douault, Wenjing Meng, Andrew Billinton, Jason Witherington, Anne Hersey, Rino A. Bit, Nick M. Clayton, James Myatt, Gianpaolo Bravi, Christopher N. Johnson, Jason D. Brown, Livermore David
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(15)
Optimization of the novel alpha-2-delta-1 ligand 4 provided compounds 37 and 38 which have improved DMPK profiles, good in vivo analgesic activity and in vitro selectivity over alpha-2-delta-2. An in-house P-gp prediction programme and the MetaSite s
Autor:
Paul Bamborough, Chun-wa Chung, RebeccaC. Furze, Paola Grandi, Anne-Marie Michon, Robert J. Sheppard, Heather Barnett, Hawa Diallo, DavidP. Dixon, Clement Douault, Emma J. Jones, Bhumika Karamshi, Darren J. Mitchell, Rab K. Prinjha, Christina Rau, RobertJ. Watson, Thilo Werner, Emmanuel H. Demont
Publikováno v:
Journal of Medicinal Chemistry; Aug2015, Vol. 58 Issue 15, p6151-6178, 28p
Autor:
Emmanuel H. Demont, Chun-wa Chung, RebeccaC. Furze, Paola Grandi, Anne-Marie Michon, Chris Wellaway, Nathalie Barrett, Angela M. Bridges, PeterD. Craggs, Hawa Diallo, David P. Dixon, Clement Douault, Amanda J. Emmons, EmmaJ. Jones, Bhumika V. Karamshi, Kelly Locke, Darren J. Mitchell, BernadetteH. Mouzon, Rab K. Prinjha, Andy D. Roberts
Publikováno v:
Journal of Medicinal Chemistry; Jul2015, Vol. 58 Issue 14, p5649-5673, 25p