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PDBsum entry 2xf0
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References listed in PDB file
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Key reference
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Title
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Design and evaluation of 3,6-Di(hetero)aryl imidazo[1,2-A]pyrazines as inhibitors of checkpoint and other kinases.
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Authors
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T.P.Matthews,
T.Mchardy,
S.Klair,
K.Boxall,
M.Fisher,
M.Cherry,
C.E.Allen,
G.J.Addison,
J.Ellard,
G.W.Aherne,
I.M.Westwood,
R.Van montfort,
M.D.Garrett,
J.C.Reader,
I.Collins.
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Ref.
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Bioorg Med Chem Lett, 2010,
20,
4045-4049.
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PubMed id
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Abstract
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A range of 3,6-di(hetero)arylimidazo[1,2-a]pyrazine ATP-competitive inhibitors
of CHK1 were developed by scaffold hopping from a weakly active screening hit.
Efficient synthetic routes for parallel synthesis were developed to prepare
analogues with improved potency and ligand efficiency against CHK1. Kinase
profiling showed that the imidazo[1,2-a]pyrazines could inhibit other kinases,
including CHK2 and ABL, with equivalent or better potency depending on the
pendant substitution. These 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines appear to
represent a general kinase inhibitor scaffold.
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Secondary reference #1
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Title
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Identification of inhibitors of checkpoint kinase 1 through template screening.
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Authors
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T.P.Matthews,
S.Klair,
S.Burns,
K.Boxall,
M.Cherry,
M.Fisher,
I.M.Westwood,
M.I.Walton,
T.Mchardy,
K.M.Cheung,
R.Van montfort,
D.Williams,
G.W.Aherne,
M.D.Garrett,
J.Reader,
I.Collins.
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Ref.
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J Med Chem, 2009,
52,
4810-4819.
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PubMed id
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