Synthesis and antitumor activity in vitro of novel berbamine derivatives.

A series of new berbamine derivatives were synthesized, and their cytotoxic activity was evaluated against Human T-cell lymphoma cell line H9 and multiple myeloma cell line RPMI8226 in vitro. Compared with berbamine, the cytotoxicity of the modified derivatives was enhanced, especially simultaneously substituted at OH and 5-position. Compounds 2a and 4b exhibited high antitumor activity. The IC50 value of compound 2a was 0.30 µM for RPMI8226 cells, and the IC50 value of compound 4b was 0.36 µM for H9 cells, whereas berbamine IC50 values were 4.0 µM for H9 cells and 6.19 µM for RPMI8226 cells, respectively.[Formula: see text].