SGI-1027 作为一种 DNA 甲基转移酶抑制剂的合成方法及其对 U937 白血病细胞系的影响。
Synthetic approaches to DNMT inhibitor SGI-1027 and effects on the U937 leukemia cell line.
机构信息
Departamento de Química Orgánica, Facultade de Química, Universidade de Vigo, 36310 Vigo, Spain.
出版信息
Bioorg Med Chem Lett. 2013 Mar 15;23(6):1631-5. doi: 10.1016/j.bmcl.2013.01.085. Epub 2013 Jan 30.
PMID:23402879
Abstract
The known DNMT inhibitor SGI-1027 4 has been synthesized using as key steps Pd-catalyzed Ar-N bond formation reactions performed in a sequential or convergent manner. In the former approach, a by-product, which corresponds to the incorporation of two units of 4-chloroquinoline, was also isolated. The biological effects of compound 4 in the U937 human leukemia cell line are also described.
摘要
已知的 DNA 甲基转移酶抑制剂 SGI-1027 4 是使用钯催化的芳基-N 键形成反应作为关键步骤合成的，这些反应以顺序或收敛的方式进行。在前一种方法中，还分离出了一种副产物，它对应于两个 4-氯喹啉单元的掺入。还描述了化合物 4 在 U937 人白血病细胞系中的生物学效应。
Zotero 插件