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    J Med Chem. 2008 Apr 10;51(7):2321-5. Epub 2008 Mar 18.

    Constrained analogues of procaine as novel small molecule inhibitors of DNA methyltransferase-1.

    Castellano S, Kuck D, Sala M, Novellino E, Lyko F, Sbardella G.

    Source

    Dipartimento di Scienze Farmaceutiche, Università degli Studi di Salerno, Via Ponte Don Melillo, 84084 Fisciano (SA), Italy.

    Abstract

    Constrained analogues of procaine were synthesized, and their inhibiting activity against DNMT1 was tested. Among them, the most potent compound, derivative 3b, was also able to induce a recognizable demethylation of chromosomal satellite repeats in HL60 human myeloid leukemia cells and thus represents a lead compound for the development of a novel class of non-nucleoside DNMT1 inhibitors.

    PMID:
    18345608
    [PubMed - indexed for MEDLINE]

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