Discovery of 2-Arylbenzoxazoles as Upregulators of Utrophin Production for the Treatment of Duchenne Muscular Dystrophy
| Autor: | Severine Danielle Poignant, Fraser J. Wilkes, Kay E. Davies, Adam G. Lambert, J Vile, P J Middleton, Francis Xavier Wilson, Peter David Johnson, Stephen Paul Wren, Carole Eliane Andree Maillol, Richard Storer, Chancellor, D Lawrence, Collin Richard Dorgan, Richard Vickers, Graham Michael Wynne, A Potter, Cristina Lecci, Paul Damien Price, Gary Nugent, O De Moor, Richard Joseph Pye, R van Well, Jonathon M. Tinsley |
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| Rok vydání: | 2011 |
| Předmět: |
Benzoxazoles
Luciferase reporter Utrophin Duchenne muscular dystrophy Naphthalenes Biology Pharmacology medicine.disease Molecular biology Cell Line Up-Regulation Muscular Dystrophy Duchenne Mice Structure-Activity Relationship Downregulation and upregulation Drug Discovery medicine Animals Molecular Medicine ADME |
| Zdroj: | Journal of Medicinal Chemistry. 54:3241-3250 |
| ISSN: | 1520-4804 0022-2623 |
| Popis: | A series of novel 2-arylbenzoxazoles that upregulate the production of utrophin in murine H2K cells, as assessed using a luciferase reporter linked assay, have been identified. This compound class appears to hold considerable promise as a potential treatment for Duchenne muscular dystrophy. Following the delineation of structure-activity relationships in the series, a number of potent upregulators were identified, and preliminary ADME evaluation is described. These studies have resulted in the identification of 1, a compound that has been progressed to clinical trials. |
| Databáze: | OpenAIRE |
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