Zobrazeno 1 - 5
of 5
pro vyhledávání: '"David G. Acton"'
Autor:
Nicola Colclough, David G. Acton, Alan Girdwood, Andrew A. Mortlock, David M. Andrews, Peter Ballard, Neil James Hales, Alfred A. Rabow, Graeme Walker, David A. Jude, Owen Jones, Nigel Brooks, Robert Hugh Bradbury, Urs Hancox, Sarah A. Loddick
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:5442-5445
Chemical starting points were investigated for downregulation of the androgen receptor as an approach to treatment of advanced prostate cancer. Although prototypic steroidal downregulators such as 6a designed for intramuscular administration showed i
Autor:
Michael B. Gravestock, Alexandra McGregor, Michael Dennis, R. Geoffrey Wilson, Lisa Woods, Alan Wookey, Michael John Betts, Glenn Hatter, Swain Michael Lingard, David G. Acton
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:4179-4186
Exploration of the structure-activity relationships of the traditional C-5 acetamidomethyl side chain of the oxazolidonone antibacterials has yielded new, potent series of compounds of which the first examples, the O-linked iosoxazoles are described
Autor:
Joanne Wilson, J. Matthew Wood, A. Nigel Brooks, Hill Kathryn Jane, Alfred A. Rabow, Graeme Walker, Andrew G. Thomason, Barry R. Hayter, Nicholas J. Howe, Stuart L. Wells, Glenn Hatter, David A. Jude, Sarah A. Loddick, Gorkhn Sharma-Singh, Scott G. Lamont, Heather L. McFarland, Dawn Trueman, Natalie Stratton, Zaieda Parveen, Nicola Broadbent, Carr Gregory Richard, David G. Acton, Robert Hugh Bradbury, Rhys D.O. Jones
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(7)
Removal of the basic piperazine nitrogen atom, introduction of a solubilising end group and partial reduction of the triazolopyridazine moiety in the previously-described lead androgen receptor downregulator 6-[4-(4-cyanobenzyl)piperazin-1-yl]-3-(tri
Autor:
David William AstraZeneca R D Alderley Heaton, Hazel M. Weir, Julie A. Tucker, Eric Fisher, Galith Karoutchi, Sarah A. Loddick, Mark A. Graham, Michael Dennis, Clive Green, Barker Andrew John, David M. Andrews, Andrew D. Roberts, M. Raymond V. Finlay, Rémy Morgentin, David G. Acton
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(15)
A piperazine series of cyclin-dependent kinase (CDK) inhibitors have been identified. The compounds exhibit excellent physiochemical properties and a novel binding mode, whereby a bridging interaction via a water molecule with Asp 86 of CDK2, leads t
Autor:
Bernard Barlaam, David G. Acton, Peter Ballard, Robert H. Bradbury, Darren Cross, Richard Ducray, Hervé Germain, Kevin Hudson, Teresa Klinowska, Françoise Magnien, Donald J. Ogilvie, Annie Olivier, Helen S. Ross, Robin Smith, Cath B. Trigwell, Michel Vautier, Lindsay Wright
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(6)
We have identified a new series of C-5 substituted indazolylaminoquinazolines as potent erbB2 kinase inhibitors. The lead compound 22 showed excellent in vitro potency, good physical properties, acceptable oral pharmacokinetics in rat and dog, and lo