Synthesis and antitumor activity of the derivatives of cephalotaxine and drupacine / 药学学报

ABSTRACT

<p><b>AIM</b>To make full use of cephalotaxus plant resources and search for antitumor agents with higher activities and lower side effects.</p><p><b>METHODS</b>The 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.</p><p><b>RESULTS</b>Six 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.</p><p><b>CONCLUSION</b>Novel alkaloid esters are worthy to be intensively studied.</p>