Title of article
Inhibitors of the tyrosine kinase EphB4. Part 2: Structure-based discovery and optimisation of 3,5-bis substituted anilinopyrimidines
Author/Authors
Catherine Bardelle، نويسنده , , Tanya Coleman، نويسنده , , Darren Cross، نويسنده , , Sara Davenport، نويسنده , , Jason G. Kettle، نويسنده , , Eun Jung Ko، نويسنده , , Andrew G. Leach، نويسنده , , Andrew Mortlock، نويسنده , , Jon Read، نويسنده , , Nicola J. Roberts، نويسنده , , Peter Robins، نويسنده , , Emma J. Williams، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
5717
To page
5721
Abstract
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.
Keywords
EphB4 , Pyrimidine , structure-based design , tyrosine kinase
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
800093
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