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    Bioorg Med Chem Lett. 2005 Oct 15;15(20):4427-31.

    Design and synthesis of phthalimide-type histone deacetylase inhibitors.

    Source

    Institute of Molecular and Cellular Biosciences, The University of Tokyo Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.

    Abstract

    Several hydroxamic acid derivatives with a substituted phthalimide group as a linker and/or cap structure, prepared during structural development studies based on thalidomide, were found to have histone deacetylase (HDAC)-inhibitory activity. Structure-activity relationship studies indicated that nature of the substituent introduced at the phthalimide nitrogen atom, introduction of a hydroxamic acid structure, and distance between the N-hydroxyl group and the cap structure are important for HDAC-inhibitory activity.

    PMID:
    16137884
    [PubMed - indexed for MEDLINE]

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