Study on the modification and anti-tumor activity of silybin derivatives for CDK4/6 targeted

VernacularTitle:靶向CDK4/6抑制剂水飞蓟宾衍生物的合成及抗肿瘤活性研究
Author: Shi-te GAO ^{1
,

2} ; Zhen-yu KUAI ³ ; Zhi-peng ZHANG ¹ ; Yan-qiu MENG ¹
Author Information

1. Shenyang University of Chemical Technology, Shenyang 110142, China
2. Shenyang Institute of Science and Technology, Shenyang 110166, China
3. Ma'anshan Vocational and Technical College, Ma'anshan 243031, China
Publication Type:Research Article
Keywords: erivative of silybin; CDK4/6 inhibitor; structural modification; anti-tumor activity
From: Acta Pharmaceutica Sinica 2023;58(3):721-728
CountryChina
Language:Chinese
Abstract: By using computer-aided drug design, the activities group model which CDK4/6 inhibitors on the market were introduced to silybin C-7, and a series of silybin derivatives were designed and synthesized, and the structure was confirmed by MS, ¹³C NMR and ¹H NMR. The in vitro antitumor activity evaluation of the target compound was carried out by MTT method, and the in vitro anti-tumor activity was carried out in human hepatocellular carcinoma cells (HepG-2). Experimental results show that all compounds are higher than the activity of the parent silybin, of which compound I₁ has a certain inhibitory effect on human HepG-2 cells, which is worth further study.