含水杨酸结构单元的黄酮衍生物设计、合成及其抗肿瘤活性研究

Design,synthesis and anti-tumor activity of flavonoid derivatives containing salicylic acid structure

目的设计合成含水杨酸结构单元的黄酮衍生物并进行体外抗肿瘤增殖活性研究。方法基于药效团拼合原理,选定黄酮类化合物作为母核结构,引入两个重要的药效活性片段(三甲氧基苯基,水杨酸),合成新型黄酮衍生物,并进行相关的抗肿瘤增殖活性研究。结果 共设计、合成得到6个目标化合物,其中化合物7f对胃癌细胞株HGC-27具有较好的抗增殖活性,IC50值为(10.26±6.94)μmol·L-1,可以有效地抑制肿瘤细胞的体外增殖生长与迁移修复能力,诱导肿瘤细胞的凋亡。结论研究结果表明化合物7f作为筛选出的目标药物,对胃癌治疗极具潜力,可为抗肿瘤治疗药物的开发提供有效的研究基础。

Objective To design and synthesize the flavonoid derivatives containing salicylic acid structure and study their antitumor activity in vitro.Methods Based on the principle of drug combination,flavones were used as the mother core,two important pharmacophores (trimethoxyphenyl and salicylic acid derivative) were combined to synthesize new types of flavonoids and study in vitro antitumor activities.Results Six new flavonoids were synthesized:compound 7f showed good anti-proliferative activity against gastric cancer cell line HGC-27 with an IC50 value of (10.26±6.94) μmol·L-1,which inhibited the colony formation and migration of tumor cells and promoted the tumor cell apoptosis.Conclusion Compound 7f,as the selected target drug may have great potential in the treatment of gastric cancer and provide an effective research basis for the development of anti-tumor drugs.