含喹啉片段的槲皮素衍生物的设计、合成及抗肿瘤活性。
Design, Synthesis and Antitumor Activity of Quercetin Derivatives Containing a Quinoline Moiety.
机构信息
Xuzhou Institute of Agricultural Sciences in Jiangsu Xuhuai District, Xuzhou 221131, China.
School of Life Sciences, Jiangsu Normal University, Xuzhou 221008, China.
出版信息
Molecules. 2024 Jan 2;29(1):240. doi: 10.3390/molecules29010240.
Quercetin is a flavonoid with significant biological and pharmacological activity. In this paper, quercetin was modified at the 3-OH position. Rutin was used as a raw material. We used methyl protection, Williamson etherification reactions, and then substitution reactions to prepare 15 novel quercetin derivatives containing a quinoline moiety. All these complexes were characterized by H NMR, C NMR, IR and HRMS. Of these, compound (IC = 6.722 μmol·L) had a better inhibitory effect on human liver cancer (HepG-2) than DDP (Cisplatin) (IC = 26.981 μmol·L). The mechanism of the action experiment showed that compound could induce cell apoptosis.
槲皮素是一种具有重要生物学和药理学活性的类黄酮。在本文中，我们对槲皮素的 3-OH 位进行了修饰。芦丁被用作原料。我们使用甲基保护、Williamson 醚化反应，然后进行取代反应，制备了 15 种含有喹啉结构的新型槲皮素衍生物。所有这些配合物都通过 H NMR、C NMR、IR 和 HRMS 进行了表征。其中，化合物 （IC = 6.722 μmol·L）对人肝癌（HepG-2）的抑制作用优于 DDP（顺铂）（IC = 26.981 μmol·L）。作用机制实验表明，化合物 可以诱导细胞凋亡。
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