1. 4-(1,3-Thiazol-2-yl)morpholine derivatives as inhibitors of phosphoinositide 3-kinase.
- Author
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Alexander R, Balasundaram A, Batchelor M, Brookings D, Crépy K, Crabbe T, Deltent MF, Driessens F, Gill A, Harris S, Hutchinson G, Kulisa C, Merriman M, Mistry P, Parton T, Turner J, Whitcombe I, and Wright S
- Subjects
- Animals, Combinatorial Chemistry Techniques, Drug Screening Assays, Antitumor, Humans, Isoenzymes, Mice, Molecular Structure, Morpholines chemical synthesis, Morpholines chemistry, Structure-Activity Relationship, Thiazoles chemical synthesis, Thiazoles chemistry, Xenograft Model Antitumor Assays, 1-Phosphatidylinositol 4-Kinase antagonists & inhibitors, Morpholines pharmacology, Thiazoles pharmacology
- 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.
- Published
- 2008
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