Design, Synthesis and Antitumor Activity of Quercetin Derivatives Containing a Quinoline Moiety

含喹啉部分的槲皮素衍生物的设计、合成及抗肿瘤活性

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Abstract

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 (1)H NMR, (13)C NMR, IR and HRMS. Of these, compound 3e (IC(50) = 6.722 μmol·L(-1)) had a better inhibitory effect on human liver cancer (HepG-2) than DDP (Cisplatin) (IC(50) = 26.981 μmol·L(-1)). The mechanism of the action experiment showed that compound 3e could induce cell apoptosis.

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