title: Inhibitors of the tyrosine kinase EphB4. Part 1: Structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines.
abstract: A series of bis-anilinopyrimidines have been identified as potent inhibitors of the tyrosine kinase EphB4. Structural information from two alternative series identified from screening efforts was combined to identify the initial leads.
authors.affiliation: AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK.
authors.forename: Catherine
authors.initials: C
authors.lastname: Bardelle
authors.forename: Darren
authors.initials: D
authors.lastname: Cross
authors.forename: Sara
authors.initials: S
authors.lastname: Davenport
authors.forename: Jason G
authors.initials: JG
authors.lastname: Kettle
authors.forename: Eun Jung
authors.initials: EJ
authors.lastname: Ko
authors.forename: Andrew G
authors.initials: AG
authors.lastname: Leach
authors.forename: Andrew
authors.initials: A
authors.lastname: Mortlock
authors.forename: Jon
authors.initials: J
authors.lastname: Read
authors.forename: Nicola J
authors.initials: NJ
authors.lastname: Roberts
authors.forename: Peter
authors.initials: P
authors.lastname: Robins
authors.forename: Emma J
authors.initials: EJ
authors.lastname: Williams
mesh_terms: D000814:Aniline Compounds / Q000138:chemical synthesis / Q000494:pharmacology*; D015195:Drug Design; D006860:Hydrogen Bonding; D007536:Isomerism; D008956:Models, Chemical; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D011743:Pyrimidines / Q000138:chemical synthesis / Q000494:pharmacology*; D036224:Receptor, EphB4 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D000814:Aniline Compounds; D047428:Protein Kinase Inhibitors; D011743:Pyrimidines; D036224:Receptor, EphB4