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Title
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Inhibitors of the tyrosine kinase EphB4. Part 2: structure-based discovery and optimisation of 3,5-bis substituted anilinopyrimidines.
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Authors
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C.Bardelle,
T.Coleman,
D.Cross,
S.Davenport,
J.G.Kettle,
E.J.Ko,
A.G.Leach,
A.Mortlock,
J.Read,
N.J.Roberts,
P.Robins,
E.J.Williams.
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Ref.
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Bioorg Med Chem Lett, 2008,
18,
5717-5721.
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PubMed id
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Abstract
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Crystallographic studies of a range of 3-substituted anilinopyrimidine
inhibitors of EphB4 have highlighted two alternative C-2 aniline conformations
and this discovery has been exploited in the design of a highly potent series of
3,5-disubstituted anilinopyrimidines. The observed range of cellular activities
has been rationalised on the basis of physicochemical and structural
characteristics.
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