Zobrazeno 1 - 10
of 31
pro vyhledávání: '"Jean-Damien Charrier"'
Autor:
Somhairle Maccormick, Steven Durrant, Anisa Nizarali Virani, Christopher John Davis, Steve Young, Golec Julian M C, Storck Pierre Henri, Philip Michael Reaper, David Kay, John Pollard, Michael O'donnell, Heather Twin, Jean-Damien Charrier, Peter Littlewood, Matthew R. Griffiths, Joanne Pinder, Ronald Knegtel
Publikováno v:
Journal of medicinal chemistry. 62(11)
The DNA damage response (DDR) is a DNA damage surveillance and repair mechanism that can limit the effectiveness of radiotherapy and DNA-damaging chemotherapy, commonly used treatment modalities in cancer. Two related kinases, ataxia telangiectasia m
Publikováno v:
Tetrahedron. 71:1515-1522
A novel approach towards the production of diverse sets of diaminopyrimidines through sequential S N Ar reactions is reported. The readily prepared 2-chloro-4-tetrafluorophenoxypyrymidine reacts regioselectively with amines at the C-2 position. The t
2-Chloro-4-tetrafluorophenoxypyrimidine: a versatile reagent for C-2 prior to C-4 functionalizations
Publikováno v:
Tetrahedron Letters. 57:1882-1884
A novel synthetic route to 2,4-functionalized pyrimidines is reported. The approach uses 2-chloro-4-tetrafluorophenoxypyrimidine, that enables sequential palladium catalyzed functionalization at the pyrimidine C-2 position, followed by S N Ar displac
Autor:
Ronald Knegtel, Jean-Damien Charrier
Publikováno v:
Expert Opinion on Drug Discovery. 8:369-381
ITK is a member of the Tec family of nonreceptor protein tyrosine kinases that plays a central role in T-cell signaling. Its inhibition is seen as an attractive approach to the treatment of immune-mediated disorders. Insight into the function of ITK
Publikováno v:
ChemInform. 47
2,4-Substituted pyrimidines are prepared by C-2 functionalization of 2-chloro-4-tetrafluorophenoxypyrimidine (I) by cross-coupling reactions followed by SNAr displacement at C-4 position with a variety of amines.
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:485-488
A novel type of caspase inhibitor prodrug that improves systemic exposure after oral administration in rats has been designed. Such a prodrug, based on a 6,6a-dihydrofuro[3,2-d]oxazol-5(3aH)-one motif, has the advantage of rapidly liberating the acti
Autor:
Paul S.H. Wang, Michael O'donnell, Alistair Rutherford, John Pollard, Jean-Damien Charrier, Somhairle Maccormick, Ronald Knegtel, Philip Michael Reaper, David Kay, Joanne Pinder, Steven Durrant, Michael Mortimore, Stephen Clinton Young, Golec Julian M C
Publikováno v:
Journal of Medicinal Chemistry. 54:2320-2330
DNA-damaging agents are among the most frequently used anticancer drugs. However, they provide only modest benefit in most cancers. This may be attributed to a genome maintenance network, the DNA damage response (DDR), that recognizes and repairs dam
Publikováno v:
Tetrahedron Letters. 55:4853-4855
A convenient, single-step, efficient synthesis of benzimidazoles from esters and diamines is reported. The methodology uses an air stable form of trimethylaluminum referred to as DABAL-Me3 and is compatible with a wide range of functional groups, inc
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
Publikováno v:
ChemInform. 46
2-Chloro-4-(2,3,5,6-tetrafluorophenoxy)pyrimidine (I) can be diaminated in a regioselective stepwise manner: first amination occurs at C-2, second amination at C-4.