N-取代腈乙基吡咯甲酰胺类化合物的制备毕业论文论文报告.doc

沈 阳 药 科 大 学 本 科 毕 业 论 文 摘 要 2 Abstract 3 第一章 前言 4 1.1 肿瘤及肿瘤的治疗 4 1.2 天然产物中抗肿瘤药物的研究进展 4 1.3 海洋生物体中的抗肿瘤药物 6 第二章 实验部分 7 2.1仪器与试剂 7 2.2目标化合物合成路线 8 2.3实验操作 8 第三章 结论 12 第四章 讨论 13 参 考 文 献 14 致 谢 15  摘 要 癌症，又称恶性肿瘤，是一种严重威胁人类健康的多发性疾病。通过化疗药物治疗肿瘤在临床研究上占据了越来越重要的地位，而在药物治疗领域中，从天然产物中寻找抗肿瘤成分的研究及对天然产物进行结构改造也越来越被人们所重视。 有机合成实验室在对吡咯吡嗪酮类药物的抗炎镇痛的研究过程中发现，一些吡咯吡嗪酮的结构类似物也具有显著的抗肿瘤的活性，并且在海洋天然产物中也发现吡咯吡嗪酮衍生物(±)Longamide和它的甲基化产物(±)Longamide methyl ester，不仅具有抗真菌的作用，也具有抗肿瘤的活性。 (±)Longamide methyl ester具有完整的吡咯吡嗪酮结构，在对它进行结构改造时，为了探讨结构对活性的影响，设计将吡嗪环打开形成一系列化合物，并设想这类化合物的两条支链链由于分子内作用，可能在构象上仍具有类似吡嗪环的结构，以期它们具有吡咯吡嗪酮类化合物类似的抗肿瘤活性。 关键词：吡咯吡嗪酮；抗肿瘤；天然产物；开链化合物  Abstract Cancer, also known as malignant tumors, is a serious multiple disease which is severe threat to human health. Chemotherapy and drug treatment as adjuvant therapy develop very fast and occupy an increasingly important position in clinical studies. So it is significant to search for anti-tumor components to make structural transformation from natural products. In the study of pyrrole-pyrazine ketones as anti-inflammatory and analgesic drug, we found that some pyrrole pyrazinone structural analogues had significant anti-tumor activity. At the same time, there are also this kind of derivatives in marine natural products (±) Longamide and (±)-Longamide methyl ester, which have not only anti-fungal action, but also anti-tumor activity. (±) Longamide methyl ester has a full pyrrole the pyrazine ketone structure. In order to investigate the influence of structure on the activity, we designed to form a series of pyrazine ring opened compounds and envisage two such compounds branched-chain effects within the molecule, may remain on the conformation of the pyrazine ring has a similar structure to pyrazine pyrrole ketone compounds which have similar anti-tumor activity. Keywords: pyrazinone pyrrole; antitumor; natural products; open-chain compound  第一章 前言 1.1 肿瘤及肿瘤的治疗 肿瘤，是机体在各种因素的作用下，局部组织的细胞在基因水平上失去了对其生长的正常调控，导致细胞的异常增长