Discovery of 2-Arylbenzoxazoles as Upregulators of Utrophin Production for the Treatment of Duchenne Muscular Dystrophy
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- 作者：Daniel R. Chancellor ; Kay E. Davies ; Olivier De Moor ; Colin R. Dorgan ; Peter D. Johnson ; Adam G. Lambert ; Daniel Lawrence ; Cristina Lecci ; Carole Maillol ; Penny J. Middleton ; Gary Nugent ; Se虂verine D. Poignant ; Allyson C. Potter ; Paul D. Price ; Richard J. Pye ; Richard Storer ; Jonathon M. Tinsley ; Renate van Well ; Richard Vickers ; Julia Vile ; Fraser J. Wilkes ; Francis X. Wilson ; Stephen P. Wren ; Graham M. Wynne
- 刊名：Journal of Medicinal Chemistry
- 出版年：2011
- 出版时间：May 12, 2011
- 年：2011
- 卷：54
- 期：9
- 页码：3241-3250
- 全文大小：1000K
- 年卷期：v.54,no.9(May 12, 2011)
- ISSN：1520-4804
文摘
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鈥揳ctivity 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.