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4-(1,3-Thiazol-2-yl)morpholine derivatives as inhibitors of phosphoinositide 3-kinase |
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| Authors: | Alexander Rikki Balasundaram Ahrani Batchelor Mark Brookings Daniel Crépy Karen Crabbe Tom Deltent Marie-France Driessens Frank Gill Andrew Harris Sue Hutchinson Gillian Kulisa Claire Merriman Mark Mistry Prakash Parton Ted Turner James Whitcombe Ian Wright Sara |
| Institution: | aDepartment of Medicinal Chemistry, UCB, 208 Bath Road, Slough, Berkshire SL1 3WE, UK;bDepartment of Biology, UCB, 208 Bath Road, Slough, Berkshire SL1 3WE, UK;cCPR&ES, UCB Pharma SA, Chemin du Foriest, 1420 Braine-l’Alleud, Belgium;dDepartment of Pharmacology, UCB, 208 Bath Road, Slough, Berkshire SL1 3WE, UK;eDepartment of DMPK, UCB, 208 Bath Road, Slough, Berkshire SL1 3WE, UK |
| 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. |
| Keywords: | PI3K Oncology Kinase inhibitor |
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