嘌呤类核苷新化合物的合成和方法学研究

项目名称： 嘌呤类核苷新化合物的合成和方法学研究

项目编号： No.20802016

项目类型： 青年科学基金项目

立项/批准年度： 2009

项目学科： 化学工业

项目作者： 郭海明

作者单位： 河南师范大学

项目金额： 20万元

中文摘要： 本项目以嘌呤为原料，分别对嘌呤的9位、6位和8位进行了一系列的修饰，发展了嘌呤核苷修饰的方法学，分别合成了手性非环核苷、9位、6位和8位分别芳基化的嘌呤、6位和8位烷基化的嘌呤及6位其它功能化的嘌呤等化合物，其中合成的新化合物达200多个，并对部分化合物进行了酪氨酸激酶抑制剂活性研究，发现7个化合物具有一定的抑制活性。共发表标注本项目编号（20802016）的论文27篇，其中SCI论文21篇，在影响因子3.0以上的期刊上发表16篇；在学术会议上交流论文27篇，被邀请报告2次；申请发明专利5项，授权3项；完成科技成果鉴定4项；获河南省自然科学优秀论文奖6项，其中一等奖3项，获得河南省教学成果特等奖1项，一等奖1项；出版教材2部。由于本项目的实施，课题负责人郭海明教授获得："教育部新世纪优秀人才计划"、"河南省学术技术带头人"、"河南省优秀青年科技专家"、"河南省青少年科技创新奖"、"河南省高校优秀共产党员"、"河南省科技创新人才杰出青年"、"全国高等院校化学专业师范生教学素质大赛优秀指导教师"等多种荣誉称号，培养硕士研究生21名，其中获得硕士学位的8名。本人也被破格遴选为博士生导师。

中文关键词： 嘌呤核苷;功能化;合成

英文摘要： The main content of this project is about the modifications of purine bases at N9, C6, C8 including the modifications of nucleosides at C6, C8 respectively. Through these researches, the methodology of modified purine bases and nucleosides was developed. The specific contents include the following aspects: i. synthesis of chiral acyclic nucleosides; ii. arylation and alkylation of purine bases and nucleosides at C6, C8; iii. other functionalizations of purine bases and nucleosides at C6 and so on. More than 200 new compounds were synthesized in this project. Some of them were treated with the tyrosine kinase and seven of them were tested to possess some tyrosine kinase inhibitor activity. Supported by the project, we train 21 graduate students, including eight students who have obtained a master's degree. At the same time, some satisfactory results were achieved, as follows: i) 27 papers were published including 21 SCI papers and the impact factor of 16 papers were above 3.0; ii) published 27 academic conference papers and did two invited reports; iii) applied 5 patents and achieved 3 authorized patents; iv) achieved 4 scientific and technological achievements appraisal; v) achieved six excellent papers of Henan Province Natural Science including three first prize and achieved one special award and one first prize of Henan Provincial Teaching Achievements; vi) published two textbooks. Due to the successful implementation of the project, the project leader, professor Haiming Guo received the following honorary titles: the Ministry of Education program for New Century Excellent Talents, Academic technology leader of Henan Province, Outstanding Youth Science and Technology expert of Henan Province, Youth Science and Technology Innovation Award of Henan Province, Excellent Communist Party Member of Henan Province, Outstanding Youth of science and technology innovation of Henan Province, Outstanding instructor of National College Chemistry Teaching Quality Competition etc. Besides, Professor Guo was selected as a PhD supervisor exceptionally.

英文关键词： purine nucleoside; functionalization; synthesis