4-(1,3-Thiazol-2-yl)morpholine derivatives as inhibitors of phosphoinositide 3-kinase.
4-(1,3-Thiazol-2-yl)morpholine derivatives have been identified as potent and selective inhibitors of phosphoinositide 3-kinase. The SAR data of selected examples are presented and the in vivo profiling of compound 18 is shown to demonstrate the utility of this class of compounds in xenograft models of tumor growth.
Alexander
Rikki
R
Department of Medicinal Chemistry, UCB, 208 Bath Road, Slough, Berkshire SL1 3WE, UK. rikki.alexander@ucb-group.com
Balasundaram
Ahrani
A
Batchelor
Mark
M
Brookings
Daniel
D
Crépy
Karen
K
Crabbe
Tom
T
Deltent
Marie-France
MF
Driessens
Frank
F
Gill
Andrew
A
Harris
Sue
S
Hutchinson
Gillian
G
Kulisa
Claire
C
Merriman
Mark
M
Mistry
Prakash
P
Parton
Ted
T
Turner
James
J
Whitcombe
Ian
I
Wright
Sara
S
D019870:1-Phosphatidylinositol 4-Kinase / Q000037:antagonists & inhibitors*; D000818:Animals; D020650:Combinatorial Chemistry Techniques; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007527:Isoenzymes; D051379:Mice; D015394:Molecular Structure; D009025:Morpholines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D023041:Xenograft Model Antitumor Assays
D007527:Isoenzymes; D009025:Morpholines; D013844:Thiazoles; D019870:1-Phosphatidylinositol 4-Kinase