PHENOLIC SUBSTITUTED LIGANDS FOR DIAGNOSIS AND THERAPY

用于诊断和治疗的酚取代配体

• 批准号: 3838069
• 负责人: M W BRECHBIEL
• 金额: --
• 依托单位: DIVISION OF CANCER TREATMENT
• 依托单位国家: 美国
• 资助国家: 美国
• 起止时间: 至
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/3838069
• 关键词: carboxylate; chelating agents; chemical binding; chemical kinetics; chemical substitution; chemical synthesis; immunoconjugates; ligands; metal complex; molecular site; neoplasm /cancer radiation therapy; neoplasm /cancer radiodiagnosis; phenols; thermodynamics

The principal objective of this project is to obtain an understanding of the fundamental coordination chemistry of polyaminocarboxylate ligands which have had one or more carboxylates replaced with a phenolate metal binding site. Thus, synthesis of a series of novel acyclic ligands of various substitution patterns is required. Information acquired from evaluation of the solution chemistry of these compounds, their kinetic and thermodynamic properties, and their serum stability may be employed to gauge the potential usefulness of the complexes in vivo. These studies will thus provide a basis for rational design of bifunctional phenolic azacarboxylate ligands for complexing metals useful as cytocidal or diagnostic agents. Further synthetic efforts to incorporate a reactive protein linking substitutent into the synthesis of the useful chelating agents would be initiated and ultimately be applied to preparing useful monoclonal antibody conjugates.

该项目的主要目标是了解 聚氨基辅助配体的基本协调化学 用一个或多个羧酸盐代替了苯甲酸酯 绑定位点。 因此，一系列新型的无环配体的合成 需要各种替代模式。 从中获取的信息 评估这些化合物的溶液化学，它们的动力学 和热力学特性及其血清稳定性 衡量体内复合物的潜在有用性。 因此，这些研究将为合理设计提供基础 双功能酚苯二羧酸盐配体，用于络合金属有用 作为胞质或诊断剂。 进一步的合成努力以结合反应性蛋白质连接 代替有用螯合剂的合成将是 启动并最终应用于准备有用的单克隆 抗体结合物。