title: 4-(1,3-Thiazol-2-yl)morpholine derivatives as inhibitors of phosphoinositide 3-kinase.
abstract: 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.
authors.affiliation: Department of Medicinal Chemistry, UCB, 208 Bath Road, Slough, Berkshire SL1 3WE, UK. rikki.alexander@ucb-group.com
authors.forename: Rikki
authors.initials: R
authors.lastname: Alexander
authors.forename: Ahrani
authors.initials: A
authors.lastname: Balasundaram
authors.forename: Mark
authors.initials: M
authors.lastname: Batchelor
authors.forename: Daniel
authors.initials: D
authors.lastname: Brookings
authors.forename: Karen
authors.initials: K
authors.lastname: Crépy
authors.forename: Tom
authors.initials: T
authors.lastname: Crabbe
authors.forename: Marie-France
authors.initials: MF
authors.lastname: Deltent
authors.forename: Frank
authors.initials: F
authors.lastname: Driessens
authors.forename: Andrew
authors.initials: A
authors.lastname: Gill
authors.forename: Sue
authors.initials: S
authors.lastname: Harris
authors.forename: Gillian
authors.initials: G
authors.lastname: Hutchinson
authors.forename: Claire
authors.initials: C
authors.lastname: Kulisa
authors.forename: Mark
authors.initials: M
authors.lastname: Merriman
authors.forename: Prakash
authors.initials: P
authors.lastname: Mistry
authors.forename: Ted
authors.initials: T
authors.lastname: Parton
authors.forename: James
authors.initials: J
authors.lastname: Turner
authors.forename: Ian
authors.initials: I
authors.lastname: Whitcombe
authors.forename: Sara
authors.initials: S
authors.lastname: Wright
mesh_terms: 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
chemical_list: D007527:Isoenzymes; D009025:Morpholines; D013844:Thiazoles; D019870:1-Phosphatidylinositol 4-Kinase