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新型呋喃木脂素衍生物的合成、手性拆分及其抗肿瘤活性研究。

Synthesis, chiral resolution, and determination of novel furan lignan derivatives with potent anti-tumor activity.

机构信息

Department of Medicinal Chemistry, College of Pharmacy, Second Military Medical University, Shanghai, People's Republic of China.

出版信息

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1961-4. doi: 10.1016/j.bmcl.2010.01.122. Epub 2010 Feb 1.

DOI:10.1016/j.bmcl.2010.01.122
PMID:20171096
Abstract

A kind of racemic furan lignans were synthesized via a novel route, and two optical isomers were obtained through a selective hydrolization. The absolute configurations were determined by circular dichroism spectroscopy after separated through a preparative column. The different activities of isomers and the racemates were evaluated on QGY-7701 and HeLa cell lines, and compound 2c showed the best activity on QGY-7701 and HeLa cell lines with IC(50) 12 microM and 13 microM, respectively.

摘要

一种外消旋呋喃木脂素通过一条新途径合成，并通过选择性水解得到两个光学异构体。通过制备柱分离后，用圆二色光谱确定了绝对构型。在 QGY-7701 和 HeLa 细胞系上评估了异构体和外消旋体的不同活性，化合物 2c 对 QGY-7701 和 HeLa 细胞系的活性最好，IC（50）分别为 12μM 和 13μM。

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