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摘要：自上世纪开始，肿瘤就威胁着人类的健康，给人类的身心造成极大的伤害。为了摆脱这一困扰，科学家们展开了抗肿瘤药物的研究，并取得了巨大的成果。CA-4类衍生物是最近几年被发现的一类新型的微管蛋白解聚因子能在低于MTD的剂量下就能使血管闭合的一类药物，目前被认为是抗肿瘤最具有发展前景的药物之一，但在实际应用中还存在较多问题。本论文通过设计合理的流程和条件，在特定的反应条件下引入磷酸酯和氨基酸烷基酯，反应得到CA-4类氨基磷酸酯化合物，以期能够得到在CA-4类似物基础上有一定改进的的抗肿瘤活性化合物。48313
毕业论文关键词：肿瘤；抗肿瘤活性；CA-4；氨基磷酸酯；
Stitching design and synthesis of CA-4 class of anticancer drugs
Abstract: Since the last century, cancer is a threat to human health, which causing great harm to the human’s physiology and psychology. In order to get rid of this problem, scientists have launched many anti-tumor drug researches, and achieved great achievements. CA-4 derivatives that in recent years were discovered as a new class of tubulin depolymerization factor can make the blood vessels closed at doses of below the MTD, it is now considered as one of the most promising anti-tumor drugs. In this paper, in order to obtaining compounds which have the antitumor activity improved on the basis of CA-4 and its analogues, the reasonable procedures and conditions was designed, and phosphoramidates of CA-4 and its analogues were synthesized by introducing phosphate ester and amino acid alkyl ester into the structure of CA-4 and its derivatives on specific reaction conditions.
Keywords: cancer; anti-tumor; CA-4; phosphoramidate
目录
1研究背景 1
1.1 抗肿瘤药物的研究背景 1
1.2 抗肿瘤药物的概述 2
1.3 抗肿瘤药物的分类 3
1.3.1 血管生成抑制剂 5
1.3.2 肿瘤血管生成抑制剂的作用特点 5
1.4 CA-4简介 5
1.4.1 CA-4的结构修饰 6
1.4.2 A、B环的改造 6
1.4.3 对CA-4二碳桥进行修饰 6
1.4.4 拼合、嵌及杂和 7
1.5 CA-4应用前景 7
1.6 本课题的研究思路及意义 8
2实验的技术路线 9
3实验方法与材料 10
3.1 实验材料 10
3.1.1 主要试剂 10
3.1.2 主要仪器 11
3.2 实验方法 11
3.2.1 分析方法 11
3.3 实验过程 12
3.3.1 [(2-甲氧基-5-甲基-((Z)-3,4,5-三甲氧基苯乙烯基)苯氧基)(苯氧基)磷酰]-l-亮氨酸甲酯（编号：5a）的制备 12
3.3.2 毛兰素的制备 13
3.3.3 [(2-甲氧基-5-甲基-((Z)-3,4,5-三甲氧基苯乙基)苯氧基)(苯氧基)磷酰]-N-Boc-L-赖氨酸甲酯（编号：6b）的制备 13
3.3.4 [(2-甲氧基-5-甲基-((Z)-3,4,5-三甲氧基苯乙基)苯氧基)(苯氧基)磷酰]-l-赖氨酸甲酯（编号：7b）的制备