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Discovery of 2-arylbenzoxazoles as upregulators of utrophin production for the treatment of Duchenne muscular dystrophy.

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Affiliations

  • 1. Summit plc , 91 Milton Park, Abingdon, Oxfordshire, OX14 4RY, United Kingdom.
      Authors
    • Chancellor DR 1
    (1 author)

ORCIDs linked to this article

Journal of Medicinal Chemistry, 15 Apr 2011, 54(9):3241-3250
https://doi.org/10.1021/jm200135z PMID: 21456623 

Abstract 

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.

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Read article at publisher's site: https://doi.org/10.1021/jm200135z

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Funding 

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Medical Research Council (1)