程家宠, 司伊康, 黄量. 几种三尖杉酯碱衍生物的合成J. 药学学报, 1983, 18(11): 835-838.
引用本文: 程家宠, 司伊康, 黄量. 几种三尖杉酯碱衍生物的合成J. 药学学报, 1983, 18(11): 835-838.
CHENG Jia-chong, SI Yi-kang , HUANG Liang, . SYNTHESIS OF SOME CEPHALOTAXINE ESTER ANALOGSJ. Acta Pharmaceutica Sinica, 1983, 18(11): 835-838.
Citation: CHENG Jia-chong, SI Yi-kang , HUANG Liang, . SYNTHESIS OF SOME CEPHALOTAXINE ESTER ANALOGSJ. Acta Pharmaceutica Sinica, 1983, 18(11): 835-838.

几种三尖杉酯碱衍生物的合成

SYNTHESIS OF SOME CEPHALOTAXINE ESTER ANALOGS

  • 摘要: 通过三尖杉碱α-酮酸酯与相应的溴代乙酸酯进行Reformatsky反应,合成了在侧链甲酯部分具有不同烷基结构的5个脱氧三尖杉酯碱衍生物。动物试验结果表明甲酯部分的甲基被其它烷基取代导致活性丧失。这又一次说明这类化合物抗癌活性的结构专属性较强。

     

    Abstract: Five deoxyharringtonine analogs with different alkyl groups in place of methyl group in the ester moiety have been synthesized by Reformatsky reaction of aketo-acyl-cephalotaxine and the corresponding alkyl bromoacetates. The results of animal test indicated that the replacement of the methyl group in the ester moiety with other alkyl groups caused loss of activity. The stringent structure specificity requirements in the antitumor activity in these series of compounds were once more demonstrated.

     

/

返回文章
返回