[三尖杉酯碱酯衍生物的合成及其抗肿瘤活性研究]
[Studies on the synthesis and antitumor activity of the derivatives of cephalotaxine alkaloid esters].
作者信息
Ye Xian-rong, Chai Yong-hai, Li Xing-nan, Wu Ke-mei
机构信息
Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
出版信息
Yao Xue Xue Bao. 2004 Jun;39(6):429-33.
AIM
To design and synthesize some cephalotaxine and drupacine derivatives with different substituentes on C3'-N of taxol side chain.
METHODS
Protective side chain acid VI (4'S,5'R) was prepared from optically active (2'R,3'S) methyl beta-phenyl glycidate I in five steps. The desired acids were coupled with cephlotaxine and drupacine respectively in the presence of 2-DPC/DMAP, followed by acidic hydrolysis and acylating to give novel alkloid esters with different substitutes on C3'-N.
RESULTS
The seven new esters were studied for antitumor activity, the results showed that the antitumor activity was influenced by the substituentes on C3'-N.
CONCLUSION
It might provide some rational basis for further structral modification.
目的
设计并合成一些在紫杉醇侧链C3'-N上带有不同取代基的三尖杉宁碱和粗榧碱衍生物。
方法
由光学活性的(2'R,3'S)β-苯基缩水甘油酸甲酯I经五步反应制备保护侧链酸VI(4'S,5'R)。所需的酸分别在2-二氯吡啶/4-二甲氨基吡啶存在下与三尖杉宁碱和粗榧碱偶联，然后进行酸水解和酰化反应，得到在C3'-N上带有不同取代基的新型生物碱酯。
结果
对这七种新酯进行了抗肿瘤活性研究，结果表明抗肿瘤活性受C3'-N上取代基的影响。
结论
这可能为进一步的结构修饰提供一些合理依据。
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