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

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• 作者：Sabrina Castellano ; Dirk Kuck ; Marina Sala ; Ettore Novellino ; Frank Lyko ; Gianluca Sbardella
• 刊名：Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：April 10, 2008
• 年：2008
• 卷：51
• 期：7
• 页码：2321 - 2325
• 全文大小：320K
• 年卷期：v.51,no.7(April 10, 2008)
• ISSN：1520-4804

文摘

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.