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.
Constrained Analogues of Procaine as Novel Small Molecule Inhibitors of DNA Methyltransferase-1 / S., Castellano; D., Kuck; Sala, Marina; Novellino, Ettore; F., Lyko; G. S. b. a. r. d. e. l. l., A.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 51:(2008), pp. 2321-2325. [10.1021/jm7015705]
Constrained Analogues of Procaine as Novel Small Molecule Inhibitors of DNA Methyltransferase-1.
SALA, MARINA;NOVELLINO, ETTORE;
2008
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.| File | Dimensione | Formato | |
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