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1. Movement disorders and the treatment of schizophrenia.

Author

Ellard, John

Subjects
*LETTERS to the editor, *SCHIZOPHRENIA, *RISPERIDONE, *ANTIPSYCHOTIC agents, *BRAIN, *CATATONIA, *CLINICAL trials, *LOGIC, *NEUROLEPTIC malignant syndrome, *TARDIVE dyskinesia, *TREATMENT effectiveness, *DEEP brain stimulation, *THERAPEUTICS, DRUG therapy for schizophrenia, THALAMUS surgery
Abstract

Presents a letter to the editor about movement disorders and the treatment of schizophrenia.

Published
2004
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2. Design and evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as inhibitors of checkpoint and other kinases

Author

Matthews, Thomas P., McHardy, Tatiana, Klair, Suki, Boxall, Kathy, Fisher, Martin, Cherry, Michael, Allen, Charlotte E., Addison, Glynn J., Ellard, John, Aherne, G. Wynne, Westwood, Isaac M., Montfort, Rob van, Garrett, Michelle D., Reader, John C., and Collins, Ian

Subjects
*DRUG design, *IMIDAZOLES, *PYRAZINES, *ADENOSINE triphosphate, *BIOSYNTHESIS, *PROTEIN kinases, *DRUG synergism, *ENZYME inhibitors, *THERAPEUTICS
Abstract

Abstract: A range of 3,6-di(hetero)arylimidazo[1,2-a]pyrazine ATP-competitive inhibitors of CHK1 were developed by scaffold hopping from a weakly active screening hit. Efficient synthetic routes for parallel synthesis were developed to prepare analogues with improved potency and ligand efficiency against CHK1. Kinase profiling showed that the imidazo[1,2-a]pyrazines could inhibit other kinases, including CHK2 and ABL, with equivalent or better potency depending on the pendant substitution. These 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines appear to represent a general kinase inhibitor scaffold. [Copyright &y& Elsevier]

Published
2010
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