富勒烯基核素促排剂的设计合成及构效关系研究

项目名称： 富勒烯基核素促排剂的设计合成及构效关系研究

项目编号： No.21301142

项目类型： 青年科学基金项目

立项/批准年度： 2014

项目学科： 数理科学和化学

项目作者： 金波

作者单位： 西南科技大学

项目金额： 24万元

中文摘要： 本项目旨在将促排性能较好的邻苯二酚和羟基吡啶酮结构键联到具有"吸收自由基的海绵"之称的富勒烯结构上，制成一种兼具促排和抗自由基双重功能的核素促排剂。通过开展富勒烯基核素促排剂的设计合成，研究富勒烯基核素促排剂的抗自由基能力及其与模拟核素Sr、Cs和U的螯合能力。建立富勒烯核素促排剂体外广谱性评价方法，并对富勒烯基核素促排剂的促排效能、抗自由基能力以及安全性进行初步评价。研究富勒烯核素促排剂结构与促排效能的关系，揭示其内在规律，提出富勒烯基核素促排剂的促排机制，为下一步设计和制备出高效的双功能广谱性核素促排剂奠定理论基础和实验依据。

中文关键词： 富勒烯；核素促排剂；抗自由基；细胞毒性；合成

英文摘要： The main research objective of this project is to synthesize bifunctional chelates for metal nuclides through the bonding of fullerene with catechol or hydroxy pyridone. The new fullerene-based bifunctional chelates possess unusual abilities of both anti-free radicals and radionuclide chelating. In this issue, first, we design and synthesize the new fullerene-based radionuclide chelating agents to study the anti-free radicals ability and the chelating abilities of fullerene-based radionuclide chelating agents with the simulated nuclide Sr, Cs and U. Second, a wide-adaptability method to evaluate the chelation ability of fullerene-based radionuclide chelating agents in vitro is established. Third, the chelation effectiveness, anti-free radical ability and security of the obtained fullerene-based radionuclide chelating agents are evaluated. The end, the relationship of chelation effectiveness and the structure of fullerene-based radionuclide chelating agents is researched , which is anticipated to provide a deeper understanding of the chelation mechanism and internal rule at the molecular level. These results offer a more valuable theoretical and experimental basis to design and prepare the efficient bifunctional wide-adaptability radionuclide chelating agents in the further research.

英文关键词： fullerene；radionuclide chelating agent；anti-free radical ability； cytotoxicity ；synthesis