Ye Xian-rong, Wu Ke-mei
Institute of Materia Medica Chinese Academy of Medical Science, Peking Union Medical College, Beijing 100050, China.
Yao Xue Xue Bao. 2003 Dec;38(12):919-23.
To make full use of cephalotaxus plant resources and search for antitumor agents with higher activities and lower side effects.
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.
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.
Novel alkaloid esters are worthy to be intensively studied.
充分利用三尖杉植物资源，寻找活性更高、副作用更低的抗肿瘤药物。
用紫杉醇侧链及其异构体对三尖杉碱和粗榧碱的C3羟基进行酰化反应，得到一系列三尖杉碱和粗榧碱的衍生物。
设计并合成了6种新型生物碱酯。药理筛选结果表明，VIIIa、VIIIb、IXa和IXc在体外对KB、HCT和Bel具有显著活性。
新型生物碱酯值得深入研究。
