新型 DNA 甲基转移酶 1 抑制剂的设计、合成、抑制活性及结合模式研究。
Design, synthesis, inhibitory activity, and binding mode study of novel DNA methyltransferase 1 inhibitors.
机构信息
Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Nagoya, Aichi 467-8603, Japan.
出版信息
Bioorg Med Chem Lett. 2010 Feb 1;20(3):1124-7. doi: 10.1016/j.bmcl.2009.12.016. Epub 2009 Dec 21.
PMID:20056538
Abstract
To identify novel non-nucleoside DNA methyltransferase (DNMT) inhibitors, we designed and synthesized a series of maleimide derivatives. Among this series, compounds 5-8 were found to be more potent DNMT1 inhibitors than RG108, a DNMT1 inhibitor reported previously by Siedlecki et al. The binding mode analysis of compound 5 is also reported.
摘要
为了鉴定新型非核苷 DNA 甲基转移酶 (DNMT) 抑制剂，我们设计并合成了一系列马来酰亚胺衍生物。在这一系列中，化合物 5-8 被发现比 Siedlecki 等人之前报道的 DNMT1 抑制剂 RG108 对 DNMT1 具有更强的抑制作用。还报告了化合物 5 的结合模式分析。
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