Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines.
The SAR and pharmacokinetic profiles of a series of multi-isoform PI3K inhibitors based on a 3,4-dihydro-2H-benzo[1,4]oxazine scaffold are disclosed.
Perry
Benjamin
B
UCB, Medicinal Chemistry, Granta Park, Great Abington, Cambridge CB21 6GS, UK. bengperry@yahoo.co.uk
Alexander
Rikki
R
Bennett
Gavin
G
Buckley
George
G
Ceska
Tom
T
Crabbe
Tom
T
Dale
Verity
V
Gowers
Lewis
L
Horsley
Helen
H
James
Lynwen
L
Jenkins
Kerry
K
Crépy
Karen
K
Kulisa
Claire
C
Lightfoot
Helen
H
Lock
Chris
C
Mack
Stephen
S
Morgan
Trevor
T
Nicolas
Anne-Lise
AL
Pitt
Will
W
Sabin
Verity
V
Wright
Sara
S
D019540:Area Under Curve; D048588:Benzoxazines / Q000737:chemistry* / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D018360:Crystallography, X-Ray / Q000379:methods; D015195:Drug Design; D006801:Humans; D007249:Inflammation; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D015394:Molecular Structure; D010078:Oxazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D019869:Phosphatidylinositol 3-Kinases / Q000378:metabolism*; D020033:Protein Isoforms; D013329:Structure-Activity Relationship
D048588:Benzoxazines; D010078:Oxazines; D020033:Protein Isoforms; D019869:Phosphatidylinositol 3-Kinases