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摘要：多梳基因( polycomb group genes,PcG)家族是果蝇发育时文持同源异形基因稳定表现的重要因子。在胚胎发育、肿瘤发生和干细胞的文持中有着重要的作用。 由荷兰癌症中心于1991年在鼠淋巴瘤中发现的Bmi-1基因( B cell-specific MLV inte-gration site-1 )是多梳基因家族中重要成员之一,参与干细胞的增殖、分化与衰老,在多种肿瘤形成过程中起重要作用。研究表明当Bmi-1蛋白过度表达时对于正常细胞有很强的致癌性，并且其对于稳定成人的干细胞群有很重要的作用。通过siRNA降低Bmi-1蛋白含量可以是试管中的癌细胞衰老或死亡并且可以提高细胞毒素剂（5-氟尿嘧啶）的敏感性。Bmi-1蛋白没有酶活性，但它却是PRC1（Polycomb抑制复合物）的关键调控器。36229
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本文发现并合成的各种化合物主要用于调控Bmi-1和Bmi-1 mRNA从而控制Bmi-1蛋白含量。通过活性测试，这些化合物都有好的活性，相信在不久的将来对于治疗多种肿瘤都有很好的帮助。
毕业论文关键词： 多梳基因；Bmi-1蛋白；siRNA；治疗肿瘤
The research of An important pharmaceutical intermediate 3-bromoacetyl-8-nitro-2-methyl-imidazo[1,2-A]pyridine
Abstract：Multi-bar gene (polycomb group genes, PcG) family is homologous to maintain stability during the development of Drosophila gene expression profiled an important factor. It plays an important role in embryonic development, tumorigenesis and stem cell maintenance in. The Netherlands Cancer Center in 1991 found in mouse lymphoma Bmi-1 gene (B cell-specific MLV inte-gration site-1) is a multi-comb one important member of the gene family involved in stem cell proliferation, differentiation and senescence It plays an important role in a variety of tumor formation. Studies have shown that when overexpressed Bmi-1 protein to normal cells have a strong carcinogen, and its stabilizing adult stem cells have a very important role. Bmi-1 by siRNA reduced protein content can be a test tube aging or death of cancer cells and can improve the sensitivity of cytotoxic agents (5-fluorouracil) is. Bmi-1 protein is no activity, but it is PRC1 (Polycomb repressive complex thereof) of key governor.
In this paper, the synthesis of various compounds discovered and is mainly used for the regulation of Bmi-1 and Bmi-1 mRNA to control Bmi-1 protein. By activity tests, these compounds have a good activity, I believe that in the near future for the treatment of a variety of tumors have very good help.
Keywords：Multi-bar gene; Bmi-1 protein; siRNA; treatment of cancer
目录 4
1 前言 1
1.1世界医药及中间体市场概况 1
1.1.1世界药品市场 1
1.1.2 世界中间体市场 1
1.2 中国医药及中间体市场概况 2
1.2.1 中国药品市场 2
1.2.2 中国中间体市场 2
1.3 重点发展的药物及其中间体 2
1.3.1 文生素类中间体[14] 2
1.3.2 含氟药物中间体 3
1.3.3 杂环类中间体[19] 4
1.3.4 手性中间体[22] 6
1.3.5 其它 7
1.4 我国医药中间体发展建议与思考 7
1.4.1 我国医药中间体企业发展建议 8
1.4.2 医药中间体开发建议 9
2 实验方案和实验路线 10
2.1 实验方案的确定 10
2.2 实验路线的确定 10
3 实验部分 11
3.1 试剂及仪器 11
3.1.1 各种实验所用的试剂 11
3.1.2 实验仪器 11
3.2 实验方法 12
3.2.1 化合物2的合成 12