查耳酮类似物的合成及抗膀胱癌作用机制研究

项目名称： 查耳酮类似物的合成及抗膀胱癌作用机制研究

项目编号： No.81072539

项目类型： 面上项目

立项/批准年度： 2011

项目学科： 化学工业

项目作者： 张雁冰

作者单位： 郑州大学

项目金额： 10万元

中文摘要： 本项目的研究主要内容是在对从植物中分离得到的新查耳酮化合物的抗膀胱癌活性研究的基础上，开展合成不同类型的查耳酮类似物，并对其抗膀胱癌的活性进行系统研究。项目得到国家自然科学基金2011年小额资助，资助金额10万元。本项目的实施时间为1年，目标任务是：合成候选的新的查耳酮类似化合物50个左右，发表学术论文2篇，其中SCI收录1篇以上，培养硕士研究生2-3名，参加相关学术会议1-2次。通过合成并经核磁、质谱等手段表征，得到系列查耳酮类似物，供活性筛选，并确定其合成方法的工艺条件；对上述化合物进行体内、体外活性测定与初步评价，进行系统的查尔酮类似物抗膀胱癌活性及其构效关系研究。本项目完成102个查耳酮类似物的合成，发表相关论文5篇，其中核心期刊1篇，会议论文4篇，并且另外一篇研究论文已投Current Cancer Drug Targe，目前正在审稿中。培养硕士研究生5名，其中1名被选被选为提前攻读博士研究生。参与课题相关的会议2次，其中1个是本项目课题组所在的团队主办的"天然产物与靶向治疗癌症的研究进展"国际会议，另外一个是：2011年中国药物化学学术会议暨中英药物化学学术会议。

中文关键词： 查尔酮类似物；合成；抗膀胱癌活性；构效关系

英文摘要： On the basis of the anti-bladder cancer activity of the chalcone compounds isolated from plants, the main content of the project research is to synthesis new chalcone derivatives and investigate their anti-bladder cancer activities. The project gets the small national natural science fund subsidy in 2011 of 100,000 yuan. The project putting time into practice is 1 year. The target mission is to: generate 50 new chalcone candidates , publish 2 academic thesises among them 1 SCI, train 2 - 3 Master degree candidates, participate in relevance academic conferences 1 - 2 time. By the fact that combining and classics examine means, such as NMR, MS spectra, get the chalcone analogue series, provide activity screening, ascertain the technological conditions composing method's; Valuation carrying out the experience and observe an inner, extracorporeal active admeasurement and first step on above-mentioned compound, the bladder cancer activity carrying out the systematic chalcone analogue resisting and their structure effect concerns research. We accomplishes 102 chalcone analogues, publishes 5 relevance thesises: 1 core journal, 4 convention thesises among them. Another piece studies has already submitted to "Current Cancer Drug Targets". We have also trained 5 Master degree candidates, among them, 1 student was chosen for a doctorate graduate ahead of time. We also participated in pertinent 2 times: One is the "International Meeting on Natural Products and Cancer Targets: Progress and Promise" and it is sponsored by the project research team. another one is: Chinese Medicinal Chemistry Symposium (CMC2011).

英文关键词： chalcone derivatives;synthetize;activity of bladder cancer;structure activity relationship