Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells

…, Y Chang, X Zhang, G Kirsch, E Novellino…

Index: Valente, Sergio; Liu, Yiwei; Schnekenburger, Michael; Zwergel, Clemens; Cosconati, Sandro; Gros, Christina; Tardugno, Maria; Labella, Donatella; Florean, Cristina; Minden, Steven; Hashimoto, Hideharu; Chang, Yanqi; Zhang, Xing; Kirsch, Gilbert; Novellino, Ettore; Arimondo, Paola B.; Miele, Evelina; Ferretti, Elisabetta; Gulino, Alberto; Diederich, Marc; Cheng, Xiaodong; Mai, Antonello Journal of Medicinal Chemistry, 2014 , vol. 57, # 3 p. 701 - 713

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Citation Number: 25

Abstract

DNA methyltransferases (DNMTs) are important enzymes involved in epigenetic control of gene expression and represent valuable targets in cancer chemotherapy. A number of nucleoside DNMT inhibitors (DNMTi) have been studied in cancer, including in cancer stem cells, and two of them (azacytidine and decitabine) have been approved for treatment of myelodysplastic syndromes. However, only a few non-nucleoside DNMTi have been ...