Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, China.
Bioorg Med Chem Lett. 2012 May 15;22(10):3418-24. doi: 10.1016/j.bmcl.2012.03.102. Epub 2012 Apr 4.
Three chemical modification methods of carboxymethylation, quaternization and hydroxypropylation were used to synthesize water-soluble chitosan derivatives. In order to study the feasibility of these chitosan derivatives as backbones of nuclear imaging agents, folic acid (FA) and Technetium-99m were introduced onto the water-soluble chitosan chains. The bifunctional chelating agent 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) was conjugated to the folate grafted chitosan derivatives for chelating with radionuclides such as (64)Cu and (68)Ga. The structures of these new ligands were characterized with multiple methods. The solubility and stability of the (99m)Tc-complexes were both favorable. Further study of their radiochemical and biological properties will be performed to evaluate the usefulness of these water-soluble chitosan derivatives for nuclear imaging agent design.
采用羧甲基化、季铵化和羟丙基化三种化学修饰方法合成了水溶性壳聚糖衍生物。为了研究这些壳聚糖衍生物作为核医学成像剂骨架的可行性，将叶酸（FA）和锝-99m 引入到水溶性壳聚糖链上。双功能螯合剂 1,4,7,10-四氮杂环十二烷-1,4,7,10-四乙酸（DOTA）被连接到叶酸接枝壳聚糖衍生物上，用于与放射性核素如（64）Cu 和（68）Ga 螯合。这些新配体的结构通过多种方法进行了表征。（99m）Tc 配合物具有良好的溶解性和稳定性。进一步研究其放射化学和生物学特性，以评估这些水溶性壳聚糖衍生物在核医学成像剂设计中的有用性。
