Inhibitors of the tyrosine kinase EphB4. Part 1: Structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines.
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.
Bardelle
Catherine
C
AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK.
Cross
Darren
D
Davenport
Sara
S
Kettle
Jason G
JG
Ko
Eun Jung
EJ
Leach
Andrew G
AG
Mortlock
Andrew
A
Read
Jon
J
Roberts
Nicola J
NJ
Robins
Peter
P
Williams
Emma J
EJ
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
D000814:Aniline Compounds; D047428:Protein Kinase Inhibitors; D011743:Pyrimidines; D036224:Receptor, EphB4