Zobrazeno 1 - 5
of 5
pro vyhledávání: '"Francoise Pierard"'
Autor:
Chau Mak, Luca Settimo, Guy Brenchley, Francoise Pierard, Andrew Miller, Dean Boyall, Philip N. Collier, Adam Tanner, Heather Twin, Clare M. Bolton, Peter Chiu, Juan-Miguel Jimenez, Shazia Keily, Elisabeth Doyle, Adam P. Curnock, Ronald Knegtel, Christopher John Davis
Publikováno v:
ACS Med Chem Lett
[Image: see text] PKCθ plays an important role in T cell biology and is a validated target for a number of disease states. A series of potent and selective PKCθ inhibitors were designed and synthesized starting from a HTS hit compound. Cell activit
Autor:
Heather Twin, Chau Mak, Francoise Pierard, Juan-Miguel Jimenez, Jeremy J. Clemens, Sam Sperry, John Studley, Andrew Miller, Dean Stamos, Andreas Termin, Philip N. Collier, Guy Brenchley, Juliana L. Asgian, Brett B. Busch, Jeffrey Abt, Sandra Lechner, Roger Heim, Tina B. Flores, Ray Gross, Dao Tran, Vadims Dvornikovs, Peggy Chiang, Timothy Coon, Sarah Hudson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:3398-3402
Extensive phase II metabolism of an advanced PKCε inhibitor resulted in sub-optimal pharmacokinetics in rat marked by elevated clearance. Synthesis of the O-glucuronide metabolite as a standard was followed by three distinct strategies to specifical
Autor:
John Pollard, Francesca Mazzei, Chau Mak, Damien Fraysse, Sanjay Patel, Sharn Ramaya, David Bebbington, John Studley, Joanne Pinder, Ronald Knegtel, Daniel Robinson, Andrew Miller, Francoise Pierard, Michael O'donnell, Alistair Rutherford, Jean-Damien Charrier, David Kay, Michael Mortimore, Simon Everitt, Hayley Binch, Golec Julian M C, James Westcott
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:3586-3592
The identification of a novel series of Aurora kinase inhibitors and exploitation of their SAR is described. Replacement of the initial quinazoline core with a pyrimidine scaffold and modification of substituents led to a series of very potent inhibi
Autor:
Damien Fraysse, Peter Chiu, Philip N. Collier, Heather Twin, Luca Settimo, Francoise Pierard, Dean Boyall, Shazia Keily, Claire M. Bolton, Christopher John Davis, Guy Brenchley, Adam P. Curnock, Jaclyn Henderson, Adam Tanner, Juan-Miguel Jimenez, Andrew Miller, Stephen Clinton Young
Publikováno v:
Journal of medicinal chemistry. 56(5)
Protein kinase C θ (PKCθ) has a central role in T cell activation and survival; however, the dependency of T cell responses to the inhibition of this enzyme appears to be dictated by the nature of the antigen and by the inflammatory environment. St
Autor:
Steven Durrant, Philip N. Collier, Andrew Miller, Joanne Pinder, David Kay, Heather Twin, Jean-Damien Charrier, Sharn Ramaya, Shazia Sadiq, Juan-Miguel Jimenez, Guy Brenchley, Francoise Pierard
Publikováno v:
HETEROCYCLES. 70:509
The synthesis and reaction of a versatile 5-pyridyl boronate is described. This intermediate can be used to synthesize a range of biologically interesting 2-(1H)-pyridones.