N-取代腈乙基吡咯甲酰胺类化物的制备-毕业论文.docxVIP

沈阳药科大学本科毕业论文论文题目: N-取代腈乙基吡咯甲酰胺类化合物的制备起止时间：2014年11月10日—2015年6月5日姓名学号：学院专业：制药工程学院应用化学专业年级班级：2011级应用化学二班指导教师：实习单位：制药工程学院有机化学教研室目录摘要2Abstract3第一章前言41.1 肿瘤及肿瘤的治疗41.2 天然产物中抗肿瘤药物的研究进展41.3 海洋生物体中的抗肿瘤药物6第二章实验部分72.1仪器与试剂72.2目标化合物合成路线82.3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AbstractCancer, 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