The invention designs and synthetizes a
lead compound by using a glycyrrhetinic
acid derivative as a carrier and being connected with
norcantharidin and a derivative thereof through ester bonds, the obtained
lead compound expects to have the advantages of having
liver targeting action, prolonging action time, reducing toxic and side effects and improving the
curative effect of resisting
liver cancer, and a model compound is provided for the research of a
liver targeting medicine for the
liver cancer. Firstly, two positions of C11 and C30 in glycyrrhetinic acid molecules are reduced and synthetized respectively, methyl ester is chemically modified into glycyrrhetinic acid (GA) and 18 alpha-glycyrrhetinic acid as well as a derivative thereof, the glycyrrhetinic acid (GA) and 18 alpha-glycyrrhetinic acid as well as the derivative thereof are used as framework molecules, through a series of reactions, the framework molecules and the
norcantharidin (NCTD) as well as a derivative thereof are condensed to form ester as a
prodrug, a
cell activity
screening test is performed on 5 object compounds, 13 object compounds in 3 series are synthetized, and structural characterization is performed on a carbon spectrum, a
hydrogen spectrum and a
mass spectrum; the influence of different concentrations of 5 object compounds on HepG2
cell proliferation of the
liver cancer is inspected by a method, results show that inhibitory action presents time-
dose dependence, and the suppression ratio of 14 mu g / mL is the highest.