Glyco-conjugation in 3--anhydroicaritine

A convenient method has been developed for the glycol-conjugation in 3-position of beta-anhydroicaritine in a reasonable yield. The structure of the 3- glycosylated beta-anhydroicaritine derivatives was confirmed to be correct by H-1 NMR, C-13 NMR and HRMS spectrum. These compounds are less soluble than icaritin, but more soluble than icariside II in CCl4. The screening results showed that compounds 12h, 12i and 12j had higher cytotoxicity to HepG2 and MCF-7 at a concentration of 50 mu M. [GRAPHICS] .