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PDBsum entry 2qhm
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References listed in PDB file
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Key reference
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Title
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Optimization of a pyrazoloquinolinone class of chk1 kinase inhibitors.
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Authors
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E.J.Brnardic,
R.M.Garbaccio,
M.E.Fraley,
E.S.Tasber,
J.T.Steen,
K.L.Arrington,
V.Y.Dudkin,
G.D.Hartman,
S.M.Stirdivant,
B.A.Drakas,
K.Rickert,
E.S.Walsh,
K.Hamilton,
C.A.Buser,
J.Hardwick,
W.Tao,
S.C.Beck,
X.Mao,
R.B.Lobell,
L.Sepp-Lorenzino,
Y.Yan,
M.Ikuta,
S.K.Munshi,
L.C.Kuo,
C.Kreatsoulas.
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Ref.
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Bioorg Med Chem Lett, 2007,
17,
5989-5994.
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PubMed id
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Abstract
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The development of 2,5-dihydro-4H-pyrazolo[4,3-c]quinolin-4-ones as inhibitors
of Chk1 kinase is described. Introduction of a fused ring at the C7/C8 positions
of the pyrazoloquinolinone provided an increase in potency while guidance from
overlapping inhibitor bound Chk1 X-ray crystal structures contributed to the
discovery of a potent and solubilizing propyl amine moiety in compound 52 (Chk1
IC(50)=3.1 nM).
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