Glyco-conjugation in 3-β-anhydroicaritine.

A convenient method has been developed for the glycol-conjugation in 3-position of β-anhydroicaritine in a reasonable yield. The structure of the 3-glycosylated β-anhydroicaritine derivatives was confirmed to be correct by 1 H NMR, 13 C NMR and HRMS spectrum. These compounds are less soluble than icaritin, but more soluble than icariside II in CCl 4 . The screening results showed that compounds 12h , 12i and 12j had higher cytotoxicity to HepG2 and MCF-7 at a concentration of 50 μM.