三尖杉酯类生物碱的半合成及结构与抗肿瘤活性的关系
STUDIES ON SEMI—SYNTHESIS OF CEPHALOTAXINE ESTERS AND CORRELATION OF THEIR STRUCTURES WITH ANTITUMOR ACTIVITY
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摘要: 报道10个氨基酸三尖杉碱醋类衍生物的半合成及抗肿瘤活性,药理实验结果表明,化合物6有显著的抗癌活性,其它化合物亦有不同程度的抗癌活性。通过化学结构与抗癌作用的比较,初步探讨了此类生物碱的构效关系。Abstract: Ten esters of cephalotaxine with amino acids possessing widely different structuralfeatures have been synthesized and tested for antitumor activity. Prelimary data showed that com-pound 6 is the most active one. However it is still less potent than harringtonine,Other syntheticesters possess varying activities at 1 0μg/ml.Preliminary structure activity relationship of these esterswas discussed.
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