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.
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.
DZ Wang, GE Ma, RS Xu Shanghai. STUDIES ON THE ALKALOIDS OF CEPHALOTAXUS Ⅸ.SEMI-SYNTHESIS OF CEPHALOTAXINE ESTERS AND THEIR ANTILEUKEMIC ACTIVITYJ. Acta Pharmaceutica Sinica, 1992, 27(3): 178-184.
Citation: DZ Wang, GE Ma, RS Xu Shanghai. STUDIES ON THE ALKALOIDS OF CEPHALOTAXUS Ⅸ.SEMI-SYNTHESIS OF CEPHALOTAXINE ESTERS AND THEIR ANTILEUKEMIC ACTIVITYJ. Acta Pharmaceutica Sinica, 1992, 27(3): 178-184.

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

STUDIES ON THE ALKALOIDS OF CEPHALOTAXUS Ⅸ.SEMI-SYNTHESIS OF CEPHALOTAXINE ESTERS AND THEIR ANTILEUKEMIC ACTIVITY

  • 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。

     

    Abstract: Harringtonine, homoharringtonine, deoxyharringtonine and isoharring-tonine isolated from Cephalotaxus plant are the esters of cephalotaxine with significantinhibitory activity against P- 388 leukemia. In this investigation seventeen new esters ofcephalotaxine type alkaloids have been synthesized. Preliminary pharmacological examina-tion showed that compounds 1, 2, 2+ 3, 6 and 8 showed similar antileukemic activity ashomoharringtonine. Compounds 4, 5, 15 and 16 showed moderate inhibitory activity.Some structure-activity correlations of these esters were discussed.

     

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