摘要:研究表明，鬼臼毒素及其衍生物是具有药理活性的一种木脂素类化合物，其药理的活性首要表现为抗肿瘤活性及抗病毒活性。虽然近年来鬼臼毒素及其衍生物已成为科学家的研究热潮，但其毒性强、副作用大的缺点在临床应用上受到了严重的阻力。为了找到疗效更加好的鬼臼毒素类药物，本论文设计将鬼臼毒素与β-苯丙氨酸合成新的鬼臼毒素衍生物。92661

方法：鬼臼毒素和β-苯丙氨酸溶于二氯甲烷，冰浴下加入DCC和DMAP并置于磁力架搅拌半小时，取出后在常温下继续搅拌四小时。通过柱层析提取产物，先配制乙酸乙酯：石油醚(75:1)洗出鬼臼毒素，再用75:1:20比例的乙酸乙酯：石油醚：氨水做洗脱剂洗出产物。将产物进行旋蒸并称量。

结论：通过氢谱和碳谱检测，验证所得产物结构与预想符合，将产物低温保存下来，准备接下来做活性检测，挑出最理想的抗肿瘤药物。

毕业论文关键词：鬼臼毒素，β-苯丙氨酸，抗癌，结构修饰，低毒

ABSTRACT：Podophyllotoxin and its derivatives are a class of lignans with significant physiologicalactivities, which are mainly anti tumor activity and antiviral activity。 Although in recent years,podophyllotoxin and its derivatives have become a research boom of scientists, but its toxicity,side effects of large shortcomings in the clinical application has been a serious resistance。 In order to find more efficient and low toxicity and good water-soluble podophyllotoxin drugs, the synthesis of podophyllotoxin and β-phenylalanine derivatives was designed in this paper。源F于K优B尔C论V文N网WwW.youeRw.com 原文+QQ752^018766

Method：Podophyllotoxin and β-phenylalanine were dissolved in dichloromethane, and DCC and DMAP were added to the ice bath and placed in a magnetic column for half an hour。 After removal, stirring was continued for four hours at room temperature。 The product was extracted by column chromatography。 Ethyl acetate: petroleum ether (100: 1) was used to wash the podophyllotoxin and the product was washed with 100: 1: 20 ratio of ethyl acetate: petroleum ether: ammonia。 The product was steamed and weighed。

Reault: Through the hydrogen spectrum and carbon spectrum detection, the structure of the product was in good agreement with the expectation。 The product is retained and ready to do the activity test for find the best derivative which can resist tumers。

Key words: Podophyllotoxin，β-Phenylalanine，Anti-cancer，Structural modification，Low toxicity

目录

抗癌药物鬼臼毒素和β-苯丙氨酸衍生物的合成及表征 4

1 前言 4

2 材料与方法 6

2。1 实验材料 6

2。1。1药品 6

2。1。2仪器 6

2。2实验部分 7

2。2。1抗癌药物鬼臼毒素与β-苯丙氨酸衍生物合成来自优O尔P论R文T网WWw.YoueRw.com 加QQ7520`18766 的预实验 7

2。2。2抗癌药物鬼臼毒素与β-苯丙氨酸衍生物合成的正式实验 7

3 结果 7

3。1目标化学物的结构式 7

3。2实验数据 8

3。3附图 9

4 讨论 9

4。1展开剂的确定 9

结论与展望