New ASGPR-targeted ligands based on glycoconjugated natural triterpenoids

Autor:	Ya. A. Ivanenkov, Sergey V. Kovalev, Elena K. Beloglazkina, E. Yu. Yamansarov, Natalia L. Klyachko, Nikolai V. Zyk, Rostislav A Petrov, Dmitry A. Skvortsov, Sergei A Evteev, Anton V Lopukhov, Alexander G. Majouga
Rok vydání:	2019
Předmět:	Betulin 010405 organic chemistry Chemistry Stereochemistry In silico General Chemistry 010402 general chemistry 01 natural sciences In vitro 0104 chemical sciences Terpene chemistry.chemical_compound Triterpenoid Betulinic acid Surface plasmon resonance spectroscopy Conjugate
Zdroj:	Russian Chemical Bulletin. 68:2331-2338
ISSN:	1573-9171 1066-5285
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::8e6f153ec852abc74a9c23a071b5973f https://doi.org/10.1007/s11172-019-2707-9 Zobrazit plný text záznamu Full text from SpringerLink