Synthesis of berbamine acetyl glycosides and evaluation of antitumor activity

► A series of berbamine (natural alkaloid) glycosides was synthesized. ► The new glycosides were evaluated for their antitumor activity in vitro. ► Most of the berbamine glycosides manifested potent cytotoxic activity. ► The most potent compound showed an IC50 of 0.30 μM against L1210 leukemia cell line.