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PDBsum entry 2bmc
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References listed in PDB file
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Key reference
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Title
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Potent and selective aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition.
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Authors
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D.Fancelli,
D.Berta,
S.Bindi,
A.Cameron,
P.Cappella,
P.Carpinelli,
C.Catana,
B.Forte,
P.Giordano,
M.L.Giorgini,
S.Mantegani,
A.Marsiglio,
M.Meroni,
J.Moll,
V.Pittalà,
F.Roletto,
D.Severino,
C.Soncini,
P.Storici,
R.Tonani,
M.Varasi,
A.Vulpetti,
P.Vianello.
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Ref.
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J Med Chem, 2005,
48,
3080-3084.
[DOI no: ]
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PubMed id
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Note In the PDB file this reference is
annotated as "TO BE PUBLISHED".
The citation details given above were identified by an automated
search of PubMed on title and author
names, giving a
percentage match of
85%.
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Abstract
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Potent and selective Aurora kinase inhibitors were identified from the
combinatorial expansion of the 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole
bi-cycle, a novel and versatile scaffold designed to target the ATP pocket of
protein kinases. The most potent compound reported in this study had an IC(50)
of 0.027 microM in the enzymatic assay for Aur-A inhibition and IC(50)s between
0.05 microM and 0.5 microM for the inhibition of proliferation of different
tumor cell lines.
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