Constrained Analogues of Procaine as Novel Small Molecule Inhibitors of DNA Methyltransferase-1

Journal of Medicinal Chemistry
2008.0

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.

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