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PDBsum entry 2c6d
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References listed in PDB file
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Key reference
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Title
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Sar and inhibitor complex structure determination of a novel class of potent and specific aurora kinase inhibitors.
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Authors
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N.M.Heron,
M.Anderson,
D.P.Blowers,
J.Breed,
J.M.Eden,
S.Green,
G.B.Hill,
T.Johnson,
F.H.Jung,
H.H.Mcmiken,
A.A.Mortlock,
A.D.Pannifer,
R.A.Pauptit,
J.Pink,
N.J.Roberts,
S.Rowsell.
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Ref.
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Bioorg Med Chem Lett, 2006,
16,
1320-1323.
[DOI no: ]
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PubMed id
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Abstract
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A novel series of 5-aminopyrimidinyl quinazolines has been developed from
anilino-quinazoline 1, which was identified in a high throughput screen for
Aurora A. Introduction of the pyrimidine ring and optimisation of the
substituents both on this ring and at the C7 position of the quinazoline led to
the discovery of compounds that are highly specific Aurora kinase inhibitors.
Co-crystallisation of one of these inhibitors with a fragment of Aurora A shows
the importance of the benzamido group in achieving selectivity.
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