 |
PDBsum entry 3c5u
|
|
|
|
References listed in PDB file
|
 |
|
Key reference
|
|
|
Title
|
|
Benzothiazole based inhibitors of p38alpha map kinase.
|
|
|
Authors
|
|
C.Liu,
J.Lin,
S.Pitt,
R.F.Zhang,
J.S.Sack,
S.E.Kiefer,
K.Kish,
A.M.Doweyko,
H.Zhang,
P.H.Marathe,
J.Trzaskos,
M.Mckinnon,
J.H.Dodd,
J.C.Barrish,
G.L.Schieven,
K.Leftheris.
|
|
|
Ref.
|
|
Bioorg Med Chem Lett, 2008,
18,
1874-1879.
[DOI no: ]
|
|
|
PubMed id
|
|
|
|
|
|
|
|
|
Abstract
|
|
|
Rational design, synthesis, and SAR studies of a novel class of benzothiazole
based inhibitors of p38alpha MAP kinase are described. The issue of metabolic
instability associated with vicinal phenyl, benzo[d]thiazol-6-yl
oxazoles/imidazoles was addressed by the replacement of the central oxazole or
imidazole ring with an aminopyrazole system. The proposed binding mode of this
new class of p38alpha inhibitors was confirmed by X-ray crystallographic studies
of a representative inhibitor (6a) bound to the p38alpha enzyme.
|
|
|
|
|
|
|
