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三尖杉酯碱类似物的合成及其抗肿瘤活性
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
作者姓名:卫东  姜芸珍  赵知中
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
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。

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.
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
Authors:D Wei  YZ Jiang  ZZ Zhao
Affiliation:Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing.
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.
Keywords:α,β-Unsaturatedester- carboxylic acid  Wittig reaction.Cephalotaxine esters  Antineoplastic. agents  α-Keto-acid
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