槲皮素-3'-O-乙基衍生物的设计、合成与抗结肠癌活性研究
Design,synthesis,and anti-colon cancer activity of quercetin-3'-O-ethyl derivatives
刘翠婷 1程卉2
作者信息
- 1. 安徽中医药大学药学院,合肥 230012;长三角药物高等研究院,江苏 南通 226133
- 2. 安徽中医药大学科研技术中心,合肥 230012
- 折叠
摘要
目的 设计和合成槲皮素-3'-OH位衍生物,初步筛选抗结肠癌活性更强的槲皮素衍生物.方法 以槲皮素为先导化合物,在槲皮素-3'-OH位连接不同长度的烷烃链,再通过酰胺键或磺酰胺键连接不同类型的片段基团,设计合成一系列槲皮素衍生物并对上述化合物进行抗肿瘤活性测试.结果 设计合成了 11个槲皮素衍生物QCT-001～QCT-011,大部分化合物都具有较好的抗肿瘤活性,其中QCT-009的抑制肿瘤活性最佳,IC50为11.25～23.25μmol·L-1.结论 通过对槲皮素-3'-OH位进行片段生长、增大分子结构的修饰策略提高槲皮素抗肿瘤活性具备一定可行性,为后续研究该类化合物的合成研究提供了实验基础.
Abstract
Objective To design and synthesize derivatives of quercetin-3'-OH with the aim of preliminary screening for quercetin derivatives displaying stronger anti-colon cancer activity.Methods Quercetin was utilized as the lead compound to connect various lengths of alkyl chains at 3'-OH position.Different types of fragment groups were linked via amide or sulfonamide bonds.A series of quercetin derivatives were designed,synthesized,and subjected to anti-tumor activity testing.Results Totally 11 quercetin derivatives QCT-001～QCT-011 were successfully designed and synthesized,with most of the compounds exhibiting good anti-tumor activity.Among them,QCT-009 demonstrated the highest inhibitory activity with an IC50 ranging from 11.25 to 23.25 μmol·L-1.Conclusion The strategy of fragment growth and structural modification at 3'-OH position of quercetin shows promise in enhancing its anti-tumor activity.This study provides an experimental foundation for further research on the synthesis of such compounds.
关键词
槲皮素/衍生物/抗肿瘤/分子对接Key words
quercetin/derivative/anti-tumor/molecular docking引用本文复制引用
出版年
2024
NETL
NSTL
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