Document Report Card

ID: ALA1142437

Journal: J Med Chem

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

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

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.

CiteXplore: 18345608

DOI: 10.1021/jm7015705