20-O-连接的喜树碱酯衍生物的合成及其抗肿瘤活性
[Synthesis and antitumor activity of 20-O-linked camptothecin ester derivatives].
作者信息
Pan Xian-dao, Liu Hong-yan, Sun Piao-yang, Zhu Cheng-gen, Yang Jing, Yuan Kai-hong, Han Rui
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 Aug;39(8):591-7.
AIM
To improve the profile of 20 (S)-camptothecin, a series of 20-O-linked camptothecin phenoxyacetic acid ester derivatives have been designed.
METHODS
These derivatives were synthesized by the method of acylation. Their chemical structures were confirmed with 1HNMR, IR, MS, and HRMS. The cytotoxicities of the compounds were tested by MTT assay. The in vivo antitumor activities of these esters were evaluated against mouse liver tumor H22 in mice.
RESULTS
Twelve derivatives of camptothecin ester are new compounds.
CONCLUSION
In vitro and in vivo antitumor activity has indicated that some derivatives appeared significantly more effective than topotecan in the H22 mouse liver tumoral model.
目的
为改善20（S）-喜树碱的性质，设计了一系列20-O-连接的喜树碱苯氧乙酸酯衍生物。
方法
通过酰化方法合成这些衍生物。用1HNMR、IR、MS和HRMS确证其化学结构。用MTT法检测化合物的细胞毒性。在小鼠体内评价这些酯对小鼠肝癌H22的抗肿瘤活性。
结果
喜树碱酯的12个衍生物为新化合物。
结论
体外和体内抗肿瘤活性表明，在H22小鼠肝癌模型中，一些衍生物比拓扑替康更有效。
Zotero 插件