Synthesis and antitumor activity of the derivatives of cephalotaxine and drupacine

AimTo make full use of cephalotaxus plant resources and search for antitumor agents with higher activities and lower side effects. MethodsThe C₃ hydroxy groups of the cephlotaxine and drupacine were acylated by taxol side chain and its isomers to give a series of derivatives of cephlotaxine and drupacine. ResultsSix novel alkaloid esters were designed and synthesized. The pharmacological screening results showed that VIIIa, VIIIb, IXa and IXc exhibited significant activities on KB, HCT and Bel in vitro. Conclusion Novel alkaloid esters are worthy to be intensively studied.