| 三尖杉酯碱类似物的合成及其抗肿瘤活性 |
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| 引用本文： | 卫东,姜芸珍,赵知中.三尖杉酯碱类似物的合成及其抗肿瘤活性[J].药学学报,1990,25(9):677-683. |
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| 作者姓名： | 卫东 姜芸珍 赵知中 |
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| 作者单位： | 中国医学科学院药物研究所，中国医学科学院药物研究所，中国医学科学院药物研究所 北京 100050，北京 100050，北京 100050 |
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| 摘 要： | 合成了新结构类型的三尖杉酯碱类似物C1Z,C2E,C3E,C4E,考察了侧链烯酯酸B1,B2,B3,B4形成时顺、反异构体的比例,发现顺式构型在酸催化下易转化成反式构型。C1E对肿瘤细胞HL-60有明显的分化诱导作用及对白血病L1210有抑制作用。
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| 关 键 词： | α-酮酸 烯酯酸 改良wittig反应 三尖杉酯碱 抗肿瘤药 |
| 收稿时间： | 1989-07-13 |
SYNTHESIS OF ANALOGS OF CEPHALOTAXINE ESTERS AND THEIR ANTITUMOR ACTIVITIES. |
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| D Wei,YZ Jiang and ZZ Zhao.SYNTHESIS OF ANALOGS OF CEPHALOTAXINE ESTERS AND THEIR ANTITUMOR ACTIVITIES.[J].Acta Pharmaceutica Sinica,1990,25(9):677-683. |
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| Authors: | D Wei YZ Jiang and ZZ Zhao |
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| Institution: | Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing. |
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| Abstract: | Four analogs of cephalotaxine esters (C1Z, C2E, C3E, C4E) were synthesized. The ratio of the Z, E isomers of the side chain alpha, beta-unsaturated ester carboxylic acids is reported. The Z isomer was easy to transform to the E isomer. Compound C1Z showed significant activity of inducing cancer cell HL-60 differentiation. It also showed inhibitory activity on Leukemia L1210. |
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| Keywords: | α β-Unsaturatedester- carboxylic acid Wittig reaction Cephalotaxine esters Antineoplastic agents α-Keto-acid |
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