New ligands for targeted delivery to the liver based on glycoconjugated natural triterpenoids are proposed. Simple chemical transformations of starting lupane triterpenes led to betulin or betulinic acid conjugates with N-acetyl-d-galactosamine linked through an isopropenyl fragment of the terpene skeleton. The obtained compounds were non-toxic in vitro to a series of cancer cell lines and normal cells. Molecular docking in silico and surface plasmon resonance spectroscopy revealed a high specificity of the synthesized glycotriterpenoids to the asialogly-coprotein receptor of hepatocytes.

中文翻译：

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基于糖共轭天然三萜类化合物的新型 ASGPR 靶向配体

提出了基于糖缀合的天然三萜类化合物靶向递送至肝脏的新配体。起始羽扇豆三萜的简单化学转化导致桦木或桦木酸缀合物与通过萜骨架的异丙烯基片段连接的 N-乙酰基-d-半乳糖胺。获得的化合物在体外对一系列癌细胞系和正常细胞无毒。硅分子对接和表面等离子体共振光谱显示合成的糖三萜类化合物对肝细胞的无唾液酸共蛋白受体具有高度特异性。