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2 results on '"Crépy K"'

1. Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines.

Author

Perry B, Alexander R, Bennett G, Buckley G, Ceska T, Crabbe T, Dale V, Gowers L, Horsley H, James L, Jenkins K, Crépy K, Kulisa C, Lightfoot H, Lock C, Mack S, Morgan T, Nicolas AL, Pitt W, Sabin V, and Wright S

Subjects
Area Under Curve, Benzoxazines pharmacology, Crystallography, X-Ray methods, Drug Design, Humans, Inflammation, Inhibitory Concentration 50, Models, Chemical, Molecular Structure, Protein Isoforms, Structure-Activity Relationship, Benzoxazines chemistry, Chemistry, Pharmaceutical methods, Oxazines chemical synthesis, Oxazines pharmacology, Phosphatidylinositol 3-Kinases metabolism
Abstract

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.

Published
2008
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2. 4-(1,3-Thiazol-2-yl)morpholine derivatives as inhibitors of phosphoinositide 3-kinase.

Author

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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