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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.

Original publication

DOI

10.1021/jm200135z

Type

Journal article

Journal

J Med Chem

Publication Date

12/05/2011

Volume

54

Pages

3241 - 3250

Keywords

Animals, Benzoxazoles, Cell Line, Mice, Muscular Dystrophy, Duchenne, Structure-Activity Relationship, Up-Regulation, Utrophin