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

作　　者：刘翠婷 程卉[2] LIU Cui-ting;CHENG Hui(School of Pharmacy,Anhui University of Chinese Medicine,Hefei 230012;Research and Technology Center,Anhui University of Chinese Medicine,Hefei 230012;Drug Research Institute of Yangtze Delta,Nantong Jiangsu 226133)

机构地区：[1]安徽中医药大学药学院,合肥230012 [2]安徽中医药大学科研技术中心,合肥230012 [3]长三角药物高等研究院,江苏南通226133

出　　处：《中南药学》2024年第12期3149-3155,共7页Central South Pharmacy

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,IC_(50)为11.25~23.25 μmol·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。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 IC_(50) 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 

分 类 号：R285[医药卫生—中药学] R283[医药卫生—中医学]