Design and synthesis of new tetrandrine derivatives and their antitumor activities

Abstract

A series of tetrandrine derivatives were designed and synthesized using Suzuki coupling reaction. Eleven targeted compounds with over 50% inhibition against HL60 and A549 human cancer cell lines at 10 μM were further evaluated for the in vitro antitumor activities by MTT or SRB assay. The biological results revealed that some compounds exhibited potent antitumor activities. Thiophene derivative 6 and acetylphenyl derivative 5 were the most active ones against HL60 and A549 cell lines, with IC₅₀ values less than 5 μM, which thus could be considered as useful candidate for further development of new antitumor agents.

Keywords:

• Tetrandrine
• Suzuki coupling
• synthesis
• antitumor activity
• structure–activity relationship