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三尖杉属植物中生物碱的研究——Ⅸ.三尖杉酯碱类似物的半合成及其抗白血病活性
引用本文:王定志,马广恩,徐任生. 三尖杉属植物中生物碱的研究——Ⅸ.三尖杉酯碱类似物的半合成及其抗白血病活性[J]. 药学学报, 1992, 27(3): 178-184
作者姓名:王定志  马广恩  徐任生
作者单位:中国科学院上海药物研究所,上海200031;*云南大学化学系,昆明650091;**中国医药研究开发中心 北京948信箱 邮政编码100083
摘    要:报道三尖杉碱的十七个新的酯类化合物的半合成及其抗肿瘤作用。药理实验结果表明1,2,2+3,6和8有显著的抗癌活性,4,5,15和16有中等的抗肿瘤作用。通过化学结构和抗肿瘤活性的比较,初步探讨了此类生物碱的构效关系。

关 键 词:三尖杉属  三尖杉酯碱类似物  抗癌活性
收稿时间:1991-03-13

Studies on the alkaloids of Cephalotaxus. IX. Semi-synthesis of cephalotaxine esters and their anti-leukemic activity]
DZ Wang,GE Ma,RS Xu Shanghai. Studies on the alkaloids of Cephalotaxus. IX. Semi-synthesis of cephalotaxine esters and their anti-leukemic activity][J]. Acta pharmaceutica Sinica, 1992, 27(3): 178-184
Authors:DZ Wang  GE Ma  RS Xu Shanghai
Affiliation:Shanghai Institute of Materia Medica, Academia Sinica.
Abstract:Harringtonine, homoharringtonine, deoxyharringtonine and isoharringtonine isolated from Cephalotaxus plant are the esters of cephalotaxine with significant inhibitory activity against P-388 leukemia. In this investigation seventeen new esters of cephalotaxine type alkaloids have been synthesized. Preliminary pharmacological examination showed that compounds 1, 2, 2 + 3, 6 and 8 showed similar antileukemic activity as homoharringtonine. Compounds 4, 5, 15 and 16 showed moderate inhibitory activity. Some structure activity correlations of these esters were discussed.
Keywords:Cephalotaxine esters  Antileukemic activity  Cephalotaxus
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