Synthesis and antitumor activity in vitro of novel berbamine derivatives

Abstract

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.

Graphical Abstract

Keywords:

• Berbamine derivatives
• C-5 substitution
• synthesis
• antitumor activity

Disclosure statement

No potential conflict of interest was reported by the authors.